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MK-467
MK-467 is a peripheral Alpha2 -adrenoceptor antagonist originated by Merck & Co. It can dose-dependently attenuate the bradycardia associated with dexmedetomidine, and shorten the sedative effect without altering its quality. Clinical for Diabetes mellitus in USA was discontinued in 1994. Uses: Diabetes mellitus. Synonyms: MK-467; MK 467; MK467; UNII-66932R910R; N-(2-((2R,12bS)-2'-oxo-1,3,4,6,7,12b-hexahydrospiro[benzofuro[2,3-a]quinolizine-2,4'-imidazolidin]-3'-yl)ethyl)methanesulfonamide hydrochloride. Grades: 98%. CAS No. 130466-38-5. Molecular formula: C20H27ClN4O4S. Mole weight: 454.98.
MK-4827 hydrochloride
Cas No. 1038915-64-8.
MK 499
MK 499, also know as L706000, has been found to be a potassium channel antagonist that has been once studied the activity in the treatment of arrhythmias. The Phase II trail of it has already been discontinued by Merck. Synonyms: L 706000; L706000; L706000; MK 499; MK499; MK499. L 706000; L-706000; L-706,000; N-[1'-(6-cyano-1,2,3,4-tetrahydronaphthalen-2-yl)-4-hydroxyspiro[3,4-dihydrochromene-2,4'-piperidine]-6-yl]methanesulfonamide. Grades: 98%. CAS No. 150481-98-4. Molecular formula: C25H29N3O4S. Mole weight: 467.58.
MK-5046
MK-5046, the first BRS-3 agonist with properties suitable for use in larger mammals, has strong selectivity when binding to BRS-3 receptor. It was developed by Merck as a new approach to the treatment of obesity and still under phase I trial.(mouse Ki = 1. Uses: Mk-5046, the first brs-3 agonist with properties suitable for use in larger mammals, has strong selectivity when binding to brs-3 receptor. Synonyms: MK5046; MK-5046; MK 5046. (2R)-1, 1, 1-trifluoro-2-(4-pyrazol-1-ylphenyl)-3-[5-[[1-(trifluoromethyl)cyclopropyl]methyl]-1H-imidazol-2-yl]propan-2-ol; MK5046peak2; SCHEMBL502524; UJINBEQCDMOAHM-GOSISDBHSA-N; KB-78904; (2R)-1, 1, 1-trifluoro-2-[4-(1H-pyrazol-1-yl)phenyl]-3-(4-{[1-(trifluorom. Grades: 95%. CAS No. 1022152-70-0. Molecular formula: C20H18F6N4O. Mole weight: 444.37.
MK-5172 hydrate
In biochemical assays, MK-5172 was effective against a panel of major genotypes and variants engineered with common resistant mutations observed in clinical studies with other NS3/4a protease inhibitors. In the replicon assay, MK-5172 demonstrated subnanomolar to low-nanomolar EC50s against genotypes 1a, 1b, and 2a. In rats, MK-5172 showed a plasma clearance of 28 ml/min/kg and plasma half-life of 1.4 hr. When dosed p.o. at 5 mg/kg, the plasma exposure of MK-5172 was good with an AUC of 0.7 uM.hr. The liver exposure of the compound was quite good (23 uM at 4 hr), and MK-5172 remained in liver 24 hr after a single p.o. 5 mg/kg dose. At 24 hr, the liver concentration of MK-5172 was 0.2 uM, which was over 25-fold higher than the IC50 in the replicon assay with 50% NHS. When dosed to dogs, MK-5172 showed low clearance of 5 ml/min/kg and a 3 hr half-life after i.v. 2 mg/kg dosing and had good plasma exposure (AUC=0.4 uM.hr) after a p.o. 1 mg/kg dose. Uses: Antiviral agents. Synonyms: (33R,35S,91R,92R,5S)-5-(tert-butyl)-N-((1R,2S)-1-((cyclopropylsulfonyl)carbamoyl)-2-vinylcyclopropyl)-17-methoxy-4,7-dioxo-2,8-dioxa-6-aza-1(2,3)-quinoxalina-3(3,1)-pyrrolidina-9(1,2)-cyclopropanacyclotetradecaphane-35-carboxamide hydrate; MK-5172; MK 5172; MK5172; Grazoprevir; Grazoprevir hydrate; trade name: Zepatier?. Grades: >98%. CAS No. 1350462-55-3. Molecular formula: C38H52N6O10S. Mole weight: 784.92.
MK-5172 potassium salt
In biochemical assays, MK-5172 was effective against a panel of major genotypes and variants engineered with common resistant mutations observed in clinical studies with other NS3/4a protease inhibitors. In the replicon assay, MK-5172 demonstrated subnanomolar to low-nanomolar EC50s against genotypes 1a, 1b, and 2a. In rats, MK-5172 showed a plasma clearance of 28 ml/min/kg and plasma half-life of 1.4 hr. When dosed p.o. at 5 mg/kg, the plasma exposure of MK-5172 was good with an AUC of 0.7 uM.hr. The liver exposure of the compound was quite good (23 uM at 4 hr), and MK-5172 remained in liver 24 hr after a single p.o. 5 mg/kg dose. At 24 hr, the liver concentration of MK-5172 was 0.2 uM, which was over 25-fold higher than the IC50 in the replicon assay with 50% NHS. When dosed to dogs, MK-5172 showed low clearance of 5 ml/min/kg and a 3 hr half-life after i.v. 2 mg/kg dosing and had good plasma exposure (AUC=0.4 uM.hr) after a p.o. 1 mg/kg dose. Synonyms: Grazoprevir potassium salt; MK5172 potassium salt; MK 5172 potassium salt. Grades: >98%. CAS No. 1206524-86-8. Molecular formula: C38H49KN6O9S. Mole weight: 804.99.
MK-5172 sodium salt
In biochemical assays, MK-5172 was effective against a panel of major genotypes and variants engineered with common resistant mutations observed in clinical studies with other NS3/4a protease inhibitors. In the replicon assay, MK-5172 demonstrated subnanomolar to low-nanomolar EC50s against genotypes 1a, 1b, and 2a. In rats, MK-5172 showed a plasma clearance of 28 ml/min/kg and plasma half-life of 1.4 hr. When dosed p.o. at 5 mg/kg, the plasma exposure of MK-5172 was good with an AUC of 0.7 uM.hr. The liver exposure of the compound was quite good (23 uM at 4 hr), and MK-5172 remained in liver 24 hr after a single p.o. 5 mg/kg dose. At 24 hr, the liver concentration of MK-5172 was 0.2 uM, which was over 25-fold higher than the IC50 in the replicon assay with 50% NHS. When dosed to dogs, MK-5172 showed low clearance of 5 ml/min/kg and a 3 hr half-life after i.v. 2 mg/kg dosing and had good plasma exposure (AUC=0.4 uM.hr) after a p.o. 1 mg/kg dose. Synonyms: Grazoprevir sodium salt; MK5172 sodium salt; MK 5172 sodium salt. Grades: >98%. CAS No. 1425038-27-2. Molecular formula: C38H49N6NaO9S. Mole weight: 788.89.
MK-5198
MK-5108 is a novel small molecule with potent inhibitory activity against Aurora-A kinase. Although most of the Aurora-kinase inhibitors target both Aurora-A and Aurora-B, MK-5108 specifically inhibited Aurora-A kinase in a panel of protein kinase assays. Inhibition of Aurora-A by MK-5108 in cultured cells induced cell cycle arrest at the G(2)-M phase in flow cytometry analysis. The effect was confirmed by the accumulation of cells with expression of phosphorylated Histone H3 and inhibition of Aurora-A autophosphorylation by immunostaining assays. MK-5108 also induced phosphorylated Histone H3 in skin and xenograft tumor tissues in a nude rat xenograft model. MK-5108 inhibited growth of human tumor cell lines in culture and in different xenograft models. Furthermore, the combination of MK-5108 and docetaxel showed enhanced antitumor activities compared with control and docetaxel alone-treated animals without exacerbating the adverse effects of docetaxel. MK-5108 is currently tested in clinical trials and offers a new therapeutic approach to combat human cancers as a single agent or in combination with existing taxane therapies. Synonyms: MK5108; MK-5108; MK 5108; VX689; VX 689; VX-689. Grades: >98%. CAS No. 1010085-13-8. Molecular formula: C22H21ClFN3O3S. Mole weight: 461.94.
MK-571 sodium salt
The sodium salt hydrate of MK-571 which is an effective antagonist of CysLT1 receptor and an inhibitor of MRP1. Uses: Bronchodilator agents. Synonyms: sodium (E) -3- ( ( (3- (2- (7-chloroquinolin-2-yl) vinyl) phenyl) ( (3- (dimethylamino) -3-oxopropyl) thio) methyl) thio) propanoate; MK-571; MK 571; MK571; MK-571 sodium salt; L-660,711; L660,711; L 660,711; L-660711; L660711; L 660711. Grades: 95%. CAS No. 115103-85-0. Molecular formula: C26H26ClN2NaO3S2. Mole weight: 537.07.
MK591
Quiflapon is a synthetic compound which specifically inhibits the activity of 5-Lox and is currently under development for the treatment of asthma. Also, Quiflapon, a leukotriene biosynthesis inhibitor, induces apoptosis in prostate cancer cells. Synonyms: Quiflapon sodium; MK-591; MK 591. Grades: >98%. CAS No. 147030-01-1. Molecular formula: C34H34ClN2NaO3S. Mole weight: 609.15.
MK6-83
MK6-83 is a transient receptor potential channel ML3 activator with EC50 value of 110 nM. It can restore endolysosomal trafficking and zinc homeostasis in lysosomes of mucolipidosis type IV mutant fibroblasts. Synonyms: MK6-83; MK6 83; MK683; 5-Methyl-N-[2-(1-piperidinyl)phenyl]-2-thiophenesulfonamide. Grades: ≥98% by HPLC. CAS No. 1062271-24-2. Molecular formula: C16H20N2O2S2. Mole weight: 336.47.
MK-7145
This active molecular is a selective renal outer medullary potassium channel (RMOK) inhibitor originated by Merck Sharp & Dohme for the treatment of hypertension and heart failure. RMOK is an ATP-dependent potassium channel that transports potassium out of cells. MK-7145 is selective against other cardiac ion channels such as Cav1.2 and Nav1.5 with IC50 value > 30 μM. MK-7145 is the first small molecule ROMK inhibitor to enter clinical development. But in Feb 2015, Merck terminated a phase I trial in Hypertension in Australia and New Zealand. Uses: Hypertension and heart failure. Synonyms: MK-7145; MK 7145; MK7145; 5,5'-((1R,1'R)-piperazine-1,4-diylbis(1-hydroxyethane-2,1-diyl))bis(4-methylisobenzofuran-1(3H)-one);1255204-85-3 (2HCl). Grades: 98%. CAS No. 1255204-84-2. Molecular formula: C26H30N2O6. Mole weight: 466.53.
MK-761
MK-761 has beta adrenoceptor antagonist and vasodilating properties in a single molecule. It has beta adrenoceptor blocking activity in the isolated cat heart papillary muscle and isolated rat atria in vitro. Uses: Mk-761 has beta adrenoceptor antagonist and vasodilating properties. Synonyms: MK-761; MK 761; MK761;(S)-2-(3-(tert-butylamino)-2-hydroxypropoxy)nicotinonitrile;2-[3-(Tert-butylamino)-2-hydroxypropoxy]pyridine-3-carbonitrile. Grades: 98%. CAS No. 65321-41-7. Molecular formula: C13H19N3O2. Mole weight: 249.31.
MK-7622
MK-7622 is a cholinesterase inhibitor under evaluation for the treatment of Alzheimer's disease. No studies have been published on this compound in the peer-reviewed literature or other publicly available documents. I. Synonyms: MK7622; MK 7622; MK-7622. Grades: 98%. CAS No. 1227923-29-6. Molecular formula: C25H25N3O2. Mole weight: 399.49.
(+)-MK-801 maleate
(-)-MK-801 maleate is a potent, selective and non-competitive N-methyl-D-aspartate (NMDA) receptor antagonist with Ki of 30.5 nM that acts at the NMDA receptor-operated ion channel as an open channel blocker. It blocks NMDA receptors in a use- and voltage-dependent manner, since the channel must open for the drug to bind inside it. It anti-convulsant and likely has dissociative anesthetic properties, but it is not used clinically for this purpose due to the discovery of brain lesions, called Olney's lesions in test rats. It were used to treat hyperalgesia in the diabetic neuropathic pain (DNP). It is used in various ischemia treatments. It has been shown to be protective in various models of ischemia as well as to inhibit behavioral sensitization to certain psychostimulants. Uses: (-)-mk-801 maleate blocks nmda receptors in a use- and voltage-dependent manner, since the channel must open for the drug to bind inside it. it were used to treat hyperalgesia in the diabetic neuropathic pain (dnp). it is used in various ischemia treatments. it has been shown to be protective in various models of ischemia as well as to inhibit behavioral sensitization to certain psychostimulants. Synonyms: (-)-MK-801 maleate; (-)-MK 801 maleate; (-)-MK801 maleate; (+)-10,11-Dihydro-5-methyl-5H-dibenzo[a,d]cyclohepten-5,10-diyldiammonium maleate;Dizocilpine maleate;(5R,10S)-(+)-5-Methyl-10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5,10-imine hydrogen maleate;Dizocilpine maleate;Dizocilpine hydrogen maleate;(+)-MK-801 hydrogen maleate. Grades: >99 %. CAS No. 77086-22-7. Molecular formula: C20H19NO4. Mole weight: 337.37.
(-)-MK 801 Maleate
MK-801 is a potent, selective and non-competitive NMDA receptor antagonist with Kd of 37.2 nM in rat brain membranes. Synonyms: (-)-MK 801 hydrogen maleate; (-)-MK 801 Maleate; (-)-MK 801 (Maleate). Grades: >98%. CAS No. 121917-57-5. Molecular formula: C16H15N.C4H4O4. Mole weight: 337.37.
MK-8033
MK8033 is a novel and specific dual ATP competitive c-Met/Ron inhibitor (IC50=1 nM Wt c-Met) under investigation as a treatment for cancer. Synonyms: MK-8033; MK 8033; MK8033. Grades: >98%. CAS No. 1001917-37-8. Molecular formula: C25H21N5O3S. Mole weight: 471.53.
MK-8033 hydrochloride
MK-8033 binds 3-fold more tightly to phosphorylated c-Met kinase domain (Kd= 3.2 nM) than to its unphosphorylated counterpart (Kd = 10.4 nM). Signigicantly, MK-8033 potently inhibits kinase activity of three oncogenic c-Met activation loop mutants, Y1230C, Y1230H, and Y1235D (IC50s ranging from 0.6 to 1 nM at 50 uM ATP) in addition to other c-Met activating mutants N1100Y and M1250T. MK-8033 potently inhibited GTL-16 proliferation with an IC50 of 582 ± 30 nM. By contrast the HCT116 cell line, which does not harbor basal c-Met activation, was not inhibited by MK-8033 (IC50 > 10000 nM) [1]. MK-8033 radiosensitized the high-c-Met-expressing EBC-1 and H1993 cells but not the low-c-Met...anized 1 h after dosing and tested for p-Met (Y1349) in tumors and MK-8033 concentrations in plasma. At 100 mg/kg,essentially complete inhibition of p-Met (Y1349) was achieved. An in vivo IC50 of 1.3 uM was deduced from the relationship between plasma MK-8033 level and Met pY1349. Treatment with escalating dosed of MK-8033 for 21 days lead to antitumor efficacies in a dose-dependent manner. Dosing at 3, 10, 30, and 100 mg/kg resulted in 22, 18, 57, and 86% tumor growth inhibition, respectively, relative to tumor from vehicle-treated mice. Synonyms: MK8033 hydrochloride; MK 8033 hydrochloride. Grades: >98%. CAS No. 1283000-43-0. Molecular formula: C25H22ClN5O3S. Mole weight: 507.99.
MK-8245
MK-8245 is a liver-targeting inhibitor of stearoyl-CoA desaturase (SCD) with IC50 of 1 nM for human SCD1 and 3 nM for both rat SCD1 and mouse SCD1, with anti-diabetic and anti-dyslipidemic efficacy. Synonyms: 4-(2-Bromo-5-fluorophenoxy)-1-[5-(2H-tetrazol-5-yl)-3-isoxazolyl]piperidine; MK-8245; MK8245; MK8245. Grades: 0.98. CAS No. 1030612-90-8. Molecular formula: C17H16BrFN6O4. Mole weight: 467.25.
MK-8245 Trifluoroacetate
MK-8245 Trifluoroacetate, a phenoxy piperidine isoxazole derivative, is a liver-targeted stearoyl-CoA desaturase (SCD) inhibitor that has the potential for treatment of dyslipidemia and diabetes. IC50: human SCD1= 1 nM; rat SCD1 and mouse SCD1= 3 nM. Uses: Antidiabetic; antidyslipidemic. Synonyms: MK-8245 Trifluoroacetate; MK 8245 Trifluoroacetate; MK8245 Trifluoroacetate; 2-[5-[3-[4-(2-bromo-5-fluorophenoxy)piperidin-1-yl]-1,2-oxazol-5-yl]tetrazol-2-yl]acetic acid;2,2,2-trifluoroacetic acid; MK-8245 (Trifluoroacetate); 1415559-41-9; 2,2,2-Trifluoroacetic acid compound with 2-(5-(3-(4-(2-bromo-5-fluorophenoxy)piperidin-1-Yl. CAS No. 1415559-41-9. Molecular formula: C19H17BrF4N6O6. Mole weight: 581.28.
MK-8617
MK-8617 is a potent and selective pan-inhibitor of Hypoxia-inducible factor prolyl hydroxylase 1-3 (HIF PHD1-3) (PHD1: IC50 = 1.0 nM; PHD2: IC50 =1.0nM; PHD3: IC50 = 14nM) commonly used for the treatment of Anemia, a disease caused by inadequate red blood cells (RBCs) or hemoglobin (Hb). Synonyms: MK-8617; MK 8617; MK8617; UNII-39RRC0G27V; 39RRC0G27V; SCHEMBL3407165; AKOS030622836; N-[bis(4-methoxyphenyl)methyl]-6-oxo-2-pyridazin-3-yl-1H-pyrimidine-5-carboxamide. Grades: 99.39 %. CAS No. 1187990-87-9. Molecular formula: C24H21N5O4. Mole weight: 443.45.
MK-8745
MK-8745 is a novel Aurora-A specific inhibitor. MK8745 induced apoptotic cell death in a p53-dependent manner when tested in vitro in cell lines of multiple lineages. Exposure of p53 wild-type cells to MK8745 resulted in the induction of p53 phosphorylation (ser15) and an increase in p53 protein expression. p53-dependent apoptosis by MK8745 was further confirmed in HCT 116 p53(-/-) cells transfected with wild-type p53. Synonyms: MK-8745; MK 8745; MK8745. Grades: 0.98. CAS No. 885325-71-3. Molecular formula: C20H19ClFN5OS. Mole weight: 431.91416.
MK-886
This active molecular is a leukotriene antagonist with the IC50 of 3 nM in human polymorphonuclear leukocytes. MK-886 also inhibits PPARα activation. Inhibition of 5-lipoxygenase-activating protein (FLAP) leads to inhibited 5-lipoxygenase (5-LOX), and this may help in treating atherosclerosis. MK-886 and Celecoxib have an inhibitory effect on the growth of pancreatic cancer cell line SW1990 and angiogenesis. In Mar 1996, an animal study had been added to the Ischaemic Heart Disease pharmacodynamics section. Uses: Ischaemic heart disease. Synonyms: MK-886; MK886; MK 886; L-663,536; L663,536; L 663,536; L-663536; L663536; L 663536; 3-[3-tert-butylsulfanyl-1-[(4-chlorophenyl)methyl]-5-propan-2-ylindol-2-yl]-2,2-dimethylpropanoic acid,L-663,536,118427-55-7( MK-886 Sodium Salt). Grades: 98%. CAS No. 118414-82-7. Molecular formula: C27H34ClNO2S. Mole weight: 472.08.
MK-886 sodium salt
MK-886 is a leukotriene inhibitor that works by blocking 5-lipoxygenase activating protein (FLAP). MK886 also inhibits PPAR alpha by a non-competitive mechanism. Uses: Lipoxygenase inhibitors. Synonyms: MK-886 sodium; MK 886 sodium; MK886 sodium; 3-[3-tert-butylsulfanyl-1-[(4-chlorophenyl)methyl]-5-propan-2-ylindol-2-yl]-2,2-dimethylpropanoate sodium salt. Grades: ≥99%. CAS No. 118427-55-7. Molecular formula: C27H33ClNO2S·Na. Mole weight: 494.1.
MK-912 hydrochloride
MK-912 is a potent new selective alpha 2-adrenergic receptor antagonist that is originated by Merck & Co for the treatment of Major depressive disorder. In Dec 1999, Phase-II clinical trials for Depression in USA was on going, but now it is discontinued. Uses: Major depressive disorder. Synonyms: MK912; MK 912; MK-912. 1',3'-dimethylspiro[1,3,4,6,7,12b-hexahydro-[1]benzofuro[2,3-a]quinolizine-2,4'-1,3-diazinane]-2'-one;hydrochloride. Grades: 98%. CAS No. 119942-70-0. Molecular formula: C20H26ClN3O2. Mole weight: 375.90.
MK 996
MK-996, an imidazopyridine derivative, has been found to be an angiotensin receptor antagonist that was once developed in the treatment of hypertension by Merck. Synonyms: MK996; MK 996; MK-996; L-159282; L 159282; L159282. CHEMBL293511; 3-((2'-(Benzoylaminosulfonyl)biphenyl-4-yl)methyl)-2-ethyl-5,7-dimethyl-3H-imidazo(4,5-b)pyridine; 3-((2'-(BENZOYLAMINOSULFONYL)BIPHENYL-4-YL)METHYL)-2-ETHYL-5,7-DIMETHYL-3H-IMIDAZO[4,5-B]PYRIDINE. Grades: 98%. CAS No. 157263-00-8. Molecular formula: C30H28N4O3S. Mole weight: 524.64.
MKT 077
MKT-077 is a cationic rhodacyanine dye. It shows antiproliferative activity against cancer cell lines with EC50s value of 1.4-2.2 μM in vitro through its ability to inhibit members of the heat shock protein 70 family of molecular chaperones. Synonyms: MKT-077; MKT 077; MKT077; FJ-776; FJ 776; FJ776; 1-Ethyl-2-[[3-ethyl-5-(3-methyl-2(3H)-benzothiazolylidene)-4-oxo-2-thiazolidinylidene]methyl]-pyridinium chloride. Grades: ≥98% by HPLC. CAS No. 147366-41-4. Molecular formula: C21H22ClN3OS2. Mole weight: 432.
ML 00253764 hydrochloride
ML 00253764 hydrochloride is a MC4 receptor antagonist with IC50 value of 320nM. It may be used to counteract the effects of cachexia in cancer patients. Synonyms: ML 00253764 hydrochloride; ML00253764 hydrochloride; ML-00253764 hydrochloride; 2-[2-[2-(5-Bromo-2-methoxyphenyl)ethyl]-3-fluorophenyl]-4,5-dihydro-2-1H-imidazole hydrochloride. Grades: ≥98% by HPLC. CAS No. 1706524-94-8. Molecular formula: C18H18BrFN2O.HCl. Mole weight: 413.71.
ML-030
ML-030, a triazolothiadiazine, is a potent PDE4 inhibitor in a cell-based cyclic nucleotide-gated cation channel biosensor assay (EC50 = 18.7 nM), with IC50 of 6.7 nM, 12.9 nM, 48.2 nM, 37.2 nM, 452 nM and 49.2 nM for PDE4A, PDE4A1, PDE4B1, PDE4B2, PDE4C1,and PDE4D2, respectively. Synonyms: ML-030; ML 030; ML030; CID-11757146; CID 11757146; CID11757146. 3-(2,5-dimethoxyphenyl)-6-(3,4-dimethoxyphenyl)-7H-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazine. CAS No. 1013750-77-0. Molecular formula: C20H20N4O4S. Mole weight: 412.46.
ML 10302 hydrochloride
ML 10302 hydrochloride is a 5-HT4 agonist with EC50 value of 4 nM. It can increase sAPPα levels in the cortex in an animal model of Alzheimer's disease and exhibit progastrokinetic effects in vivo. Synonyms: ML-10302 HCl; ML-10302; ML 10302; ML10302. 4-Amino-5-chloro-2-methoxybenzoic acid 2-(1-piperidinyl)ethyl ester hydrochloride. Grades: ≥99% by HPLC. CAS No. 186826-17-5. Molecular formula: C15H21ClN2O3.HCl. Mole weight: 349.25.
ML-115
ML-115 is a potent, cell-permeable STAT3 activator with EC50 value of 2 nM. It is inactive against the related STAT1 and NFκB anti-targets. ML-115 exhibits no cytotoxicity in the parental cell lines in the STAT3 assay (HT-1080) and STAT1 assay (NIH-3T3). Synonyms: ML115; ML 115; 3-Isoxazolecarboxamide, N-(4-chloro-2,5-dimethoxyphenyl)-5-cyclopropyl-; N-(4-Chloro-2,5-dimethoxyphenyl)-5-cyclopropyl-3-isoxazolecarboxamide. Grades: ≥98%. CAS No. 912798-42-6. Molecular formula: C15H15ClN2O4. Mole weight: 322.74.
ML 120B dihydrochloride
ML 120B dihydrochloride is an ATP-competitive IKK2-selective inhibitor with IC50 value of 60 nM at 50 μM ATP. It can inhibit paw swelling, bone and cartilage degradation. Synonyms: ML 120B dihydrochloride; ML120B dihydrochloride; ML-120B dihydrochlorideN-(6-Chloro-7-methoxy-9H-pyrido[3,4-b]indol-8-yl)-2-methyl-3-pyridinecarboxamide dihydrochloride. Grades: ≥98% by HPLC. CAS No. 1782573-78-7. Molecular formula: C19H15ClN4O2.2HCl. Mole weight: 439.72.
ML-148
ML-148 is a potent and selective inhibitor of 15-hydroxy prostaglandin dehydrogenase (15-PGDH). Synonyms: ML 148; ML148; [1-(3-methylphenyl)benzimidazol-5-yl]-piperidin-1-ylmethanone. Grades: ≥98%. CAS No. 451496-96-1. Molecular formula: C20H21N3O. Mole weight: 319.4.
ML 190
ML 190 is a κ opioid receptor antagonist with IC50 value of 120 nM. Synonyms: ML 190; ML190; ML-190; N-[3-[4-(4-Methoxyphenyl)-1-piperazinyl]propyl]-1-methyl-6-oxopyrido[2,3-e]pyrrolo[1,2-a]pyrazine-5(6H)-acetamide. Grades: ≥98% by HPLC. CAS No. 1355244-02-8. Molecular formula: C27H32N6O3. Mole weight: 488.58.
(±)-ML 209
(±)-ML 209 is a RORγt inverse agonist with IC50 value of 460 nM. It has the potential to treat TH17-related autoimmune diseases. Synonyms: (±)-ML 209; (±)-ML209; (±)-ML-209; 3-(1,3-Benzodioxol-5-yl)-1-(cis-3,5-dimethyl-1-piperidinyl)-3-(2-hydroxy-4,6-dimethoxyphenyl)-1-propanone. Grades: ≥98% by HPLC. CAS No. 1334526-14-5. Molecular formula: C25H31NO6. Mole weight: 441.52.
ML213
ML213 is a selective activator of KCNQ2 (Kv7.2) and KCNQ4 (Kv7.4) with > 80-fold selectivity against other related K+ channels, and enhances Kv7.2 and Kv7.4 channels with EC50s of 230 and 510 nM, respectively. Synonyms: N-(2, 4, 6-trimethylphenyl)bicyclo[2. 2. 1]heptane-3-carboxamide; N-mesitylbicyclo[2.2.1]heptane-2-carboxamide; ML213; ML 213; ML-213; CID-3111211; CID 3111211; CID3111211; AK174864; N-(2,4,6-Trimethylphenyl)-bicyclo[2.2.1]heptane-2-carboxamide. CAS No. 489402-47-3. Molecular formula: C17H23NO. Mole weight: 257.37.
ML 218 hydrochloride
ML 218 hydrochloride is a T-type calcium channel inhibitor with IC50 values of 270 nM for Cav3.3 and 310 nM for Cav3.2. It has potential applications for the treatment of pain. Synonyms: ML218; ML 218; ML-218. 3,5-Dichloro-N-[[(1α,5α,6-exo,6α)-3-(3,3-dimethylbutyl)-3-azabicyclo[3.1.0]hex-6-yl]methyl]-benzamide hydrochloride. Grades: ≥99% by HPLC. CAS No. 1346233-68-8. Molecular formula: C19H26Cl2N2O.HCl. Mole weight: 405.79.
ML 221
ML 221 is an apelin receptor antagonist with IC50 values of 0.70μM in a cAMP assay and 1.75 μM in β-arrestin assay. It has the potential to be used to treat or mediate the homeostasis of the cardiovascular system. Synonyms: ML221; ML 221; ML-221. 5-[(4-Nitrobenzoyl)oxy]-2-[(2-pyrimidinylthio)methyl]-4H-pyran-4-one. Grades: ≥99% by HPLC. CAS No. 877636-42-5. Molecular formula: C17H11N3O6S. Mole weight: 385.35.
ML224
ML224, a TSHR inverse agonist, has been found to reduce serum free T4 and thyroperoxidase in mice in in vivo study. IC50: 2.3 uM. Uses: Ml224 is a tshr inverse agonist that has been found to reduce serum free t4 and thyroperoxidase in mice in in vivo study. Synonyms: ML224; ML-224; ML 224; NCGC00242364; NCGC-00242364; NCGC 00242364; ANTAG3; ANTAG-3; ANTAG 3; MLS003370609; SCHEMBL14151304; CS-3824; NCGC00242364-01. Grades: 98%. CAS No. 1338824-21-7. Molecular formula: C31H31N3O5. Mole weight: 525.59.
ML228
HIF pathway activator (EC50 values are 1.23 and 1.4 μM for HRE gene reporter assay and HIF-1α nuclear translocation assay respectively); acts via chelation of iron, independently of PHD. Also exhibits > 80% inhibition of the human A3 receptor, dopamine transporter, μ receptor, hERG and 5-HT2B receptor, and rat sodium channel site 2, at a concentration of 10 μM. Synonyms: ML-228; ML 228; ML228; CID-46742353; CID 46742353; CID46742353. Grades: >98%. CAS No. 1357171-62-0. Molecular formula: C27H21N5. Mole weight: 415.49.
ML 233
ML-233 is a novel apelin receptor agonist with EC50 value of 3.7 μM. Synonyms: ML 233; ML233; ML-233; (E)-4-Methyl-5-(((phenylsulfonyl)oxy)imino)-[1,1'-bi(cyclohexane)]-3,6-dien-2-one. Grades: ≥98% by HPLC. CAS No. 2080311-92-6. Molecular formula: C19H21NO4S. Mole weight: 359.44.
ML252
ML252 is a selective and brain penetrant KCNQ2 inhibitor (Kv7.2; IC50 value 69 nM) used in vivo to study KCNQ2 pharmocology. Synonyms: AOB1824; ML252; AOB 1824; ML 252; AOB-1824; ML-252; (2S)-2-phenyl-N-(2-pyrrolidin-1-ylphenyl)butanamide hydrochloride. Grades: 99%. CAS No. 1392494-64-2. Molecular formula: C20H24N2O.HCl. Mole weight: 344.88.
ML277
ML277, a sulfonylpiperidine compound, has been found to be a KCNQ1 K+ channel activator and could be used in the study of the activity of K+ channel in human cardiomyocytes. IC50: 270 nM (EC50). Uses: Ml277 has been found to be a kcnq1 k+ channel activator and could be used in the study of the activity of k+ channel in human cardiomyocytes. Synonyms: ML277; ML 277; ML-277; CHEMBL2070953; (2R)-N-[4-(4-methoxyphenyl)-1,3-thiazol-2-yl]-1-(4-methylphenyl)sulfonylpiperidine-2-carboxamide; ML 277; 1401242-74-7; MLS003875054. Grades: 98%. CAS No. 1401242-74-7. Molecular formula: C23H25N3O4S2. Mole weight: 471.59.
ML 289
ML-289 is a negative allosteric modulator of mGlu3 with IC50 value of 0.66 μM. It displays 15-fold selectivity over mGlu2 and inactivity against mGlu5.1. Synonyms: VU0463597, VU 0463597, VU-0463597, ML-289, ML 289; ML289; [ (3R) -3- (Hydroxymethyl) -1-pipridinyl][4-[2- (4-methoxyphenyl) ethynyl]phenyl]methanone. Grades: ≥98% by HPLC. CAS No. 1382481-79-9. Molecular formula: C22H23NO3. Mole weight: 349.42.
ML-298
ML-298 is a potent inhibitor of phospholipase D2 (PLD2) displaying selectivity for PLD2 over PLD1 with IC50 values of 355 and 20000 nM, respectively. Synonyms: ML 298; ML298; 3,4-Difluoro-N-[2-[1-(3-fluorophenyl)-4-oxo-1,3,8-triazaspiro[4.5]decan-8-yl]ethyl]benzamide. Grades: ≥98%. CAS No. 1426916-02-0. Molecular formula: C22H23F3N4O2. Mole weight: 432.4.
ML 298 hydrochloride
ML 298 hydrochloride is a phospholipase D2 inhibitor with IC50 values are 355 for PLD2 and >20,000 nM for PLD1. It can decrease invasive migration in U87-MG glioblastoma cells. Synonyms: ML 298 hydrochloride; ML298 hydrochloride; ML-298 hydrochloride; 3,4-Difluoro-N-[2-[1-(3-fluorophenyl)-4-oxo-1,3,8-triazaspiro[4.5]dec-8-yl]ethyl]benzamide hydrochloride. Grades: ≥98% by HPLC. Molecular formula: C22H23F3N4O2.HCl. Mole weight: 468.9.
ML-299
ML-299 is an allosteric, dual inhibitor of PLD1/PLD2 with IC50 values of 6 and 20 nM, respectively. It can be used as a probe for detecting PLD1 and PLD2 function in vitro and in vivo. Synonyms: ML 299; ML299; CID 56593087; 4-Bromo-N-[(2S)-1-[1-(3-fluorophenyl)-4-oxo-1,3,8-triazaspiro[4.5]decan-8-yl]propan-2-yl]benzamide. Grades: ≥95%. CAS No. 1426916-00-8. Molecular formula: C23H26BrFN4O2. Mole weight: 489.4.
ML-309 hydrochloride
ML-309 is a potent and selective inhibitor of mutant isocitrate dehydrogenase 1 (IDH1). It reduces 2-hydroxyglutarate production in U87 MG glioblastoma cells. Synonyms: ML 309 hydrochloride; ML309 hydrochloride; ML-309 HCl; 2-(N-[2-(benzimidazol-1-yl)acetyl]-3-fluoroanilino)-N-cyclopentyl-2-(2-methylphenyl)acetamide hydrochloride. Grades: ≥98%. CAS No. 1355327-02-4. Molecular formula: C29H29FN4O2·HCl. Mole weight: 521.
ML311
ML311, also known as EU-5346, is a potent and selective inhibitor of the Protein-Protein Interaction of Mcl-1 and Bim. EU-5346 inhibits proliferation of Her2-positive BC cells in a dose-dependent manner. ML311 is a useful tool for studying lymphoid tumorigenesis and to demonstrate the potential for using this strategy in therapies intended to bypass apoptosis resistance pathways that are activated in drug-resistant tumors. Synonyms: 7-[ (4-Ethylpiperazin-1-yl) -[4- (trifluoromethyl) phenyl]methyl]quinolin-8-ol; ML311; ML-311; ML 311; EU-5346; EU 5346; EU5346. CAS No. 315698-17-0. Molecular formula: C23H24F3N3O. Mole weight: 415.46.
ML-314
Medicinal chemistry optimization of MLS-0233108 led to ML314, the most potent molecule in this second series that exhibited full agonist behavior (100 %) on NTR1 (EC50 = 1.9 μM). ML314 showed good selectivity against NTR2 and GPR35, but did not stimulate Ca2+ mobilization. ML314 is potentially a biased agonist operating via the β-arrestin pathway rather than the traditional Gq coupled pathway. Signaling mediated by β-arrestin has distinct biochemical and functional consequences that may lead to physiological advantages as described below. This probe report describes the discovery and properties of ML301 and summarizes the HTS and follow-up campaign, which identified ML314. Synonyms: ML 314; ML-314; ML314. Grades: 0.98. CAS No. 1448895-09-7. Molecular formula: C24H28N4O3. Mole weight: 420.513.
ML 315 hydrochloride
ML 315 hydrochloride is a cdc2-like kinase and DYRK kinase inhibitor with IC50 values of 68, 68 and 231 nM for Clk1, Clk4 and Clk2 and 282 and 1156 nM for Dyrk1A and Dyrk1B. Synonyms: ML 315 hydrochloride; ML315 hydrochloride; ML-315 hydrochloride; 5-(1,3-Benzodioxol-5-yl)-N-[(3,5-dichlorophenyl)methyl]-4-pyrimidinamine hydrochloride. Grades: ≥98% by HPLC. CAS No. 1440251-53-5. Molecular formula: C18H13Cl2N3O2.HCl. Mole weight: 410.68.
ML-323
ML323 is a reversible and potent USP1-UAF1 inhibitor with IC50 vallue of 76 nM in a Ub-Rho assay and 174 nM and 820 nM in orthogonal gel-based assays using K63-linked diubiquitin (di-Ub) and monoubiquitinated PCNA (Ub-PCNA) as substrates, respectively. Synonyms: ML-323; ML 323; ML323. CAS No. 1572414-83-5. Molecular formula: C23H24N6. Mole weight: 384.487.
ML 324 dihydrochloride
ML 324 dihydrochloride is an inhibitor of Jumonji domain-containing protein 2 (JMJD2) histone demethylase. It potently suppresses herpes simplex virus (HSV) IE gene expression and viral reactivation from latency. Synonyms: ML 324 dihydrochloride; ML324 dihydrochloride; ML-324 dihydrochloride; N-[3-(dimethylamino)propyl]-4-(8-hydroxy-6-quinolinyl)-benzamide dihydrochloride. Grades: 99%. Molecular formula: C21H23N3O2.2HCl. Mole weight: 422.35.
ML 334
ML 334 is an inhibitor of Keap1-Nrf2 interaction. It can affect the cytoprotective responses to oxidative and electrophilic stress. Synonyms: ML 334; ML334; ML-334; (1S, 2R) -2- [ [ (1S) -1- [ (1, 3-Dihydro-1, 3-dioxo-2H-isoindol-2-yl) methyl] -3, 4-dihydro-2 (1H) -isoquinolinyl] carbonyl] cyclohexanecarboxylic acid. Grades: ≥98% by HPLC. CAS No. 1432500-66-7. Molecular formula: C26H26N2O5. Mole weight: 446.5.
ML-335
ML-335 is a potent and selective TREK-1/2 activator with EC50 values of 14.3 μM and 5.2 μM, respectively. Synonyms: ML 335; ML335; N-[(2,4-Dichlorophenyl)methyl]-4-[(methylsulfonyl)amino]benzamide. Grades: ≥98% by HPLC. CAS No. 825658-06-8. Molecular formula: C15H14Cl2N2O3S. Mole weight: 373.25.
ML337
ML337 is a Selective negative allosteric modulator of mGlu3 with IC50 value of 593 nM. It shows no activity at mGlu1, mGlu2 or mGlu4-8 at concentrations up to 30 μM. ML337 is a best-in-class probe for studying non-competitive antagonism of mGlu3. Uses: In vitro and in vivo probe for studying non-competitive antagonism of mglu3. Synonyms: CHEMBL2385886; ML337; ML 337; ML-337; MLS004580699; GTPL8765;(R)-(2-fluoro-4-((4-methoxyphenyl)ethynyl)phenyl)(3-hydroxypiperidin-1-yl)methanone. Grades: 98%. CAS No. 1443118-44-2. Molecular formula: C21H20FNO3. Mole weight: 353.39.
ML346
ML346, a barbituric acid skeleton compound, is a novel activator of Hsp70 which could induce HSF-1-dependent chaperone expression and repair protein folding in both cellular and animal models. It has no obvious cytotoxicity and shows some extent of specif. Uses: Ml346 is a novel activator of hsp70 which could induce hsf-1-dependent chaperone expression and repair protein folding in both cellular and animal models. Synonyms: ML346; ML-346; ML 346; ZINC00244844; AC1LG9A8; Ambcb5772104; MLS004711999; SCHEMBL13317556. Grades: 95%. CAS No. 100872-83-1. Molecular formula: C14H12N2O4. Mole weight: 272.26.
ML348
ML348, also known as CID 3238952 or SID 160654487, is a selective and reversible lysophospholipase 1 (LYPLA1) inhibitor (IC50 = 210 nM). It is 14-fold selective for LYPLA1 over LYPLA2 (IC50 = >3,000) and demonstrates little activity against a panel of more than 20 other serine hydrolases (IC50s = >10,000). Synonyms: N-[2-chloro-5-(trifluoromethyl)phenyl]-4-(2-furanylcarbonyl)-1-piperazineacetamide; ML348; ML-348; ML 348; CID 3238952; SID 160654487. CAS No. 899713-86-1. Molecular formula: C18H17ClF3N3O3. Mole weight: 415.79.
ML 351
ML 351 is a potent and selective inhibitor of 12/15-lipoxygenase (IC50 value 200 nM against human 12/15-LOX), which catalyzes the oxidation of polyunsaturated fatty acids to produce unsaturated fatty acid hydroperoxides. Studies indicate that ML351 is protective against oxidative glutamate toxicity in mouse neuronal HT22 cells, and reduces infarct size following permanent focal ischemia in a mouse model of ischemic stroke. Synonyms: ML 351; ML-351; ML351; CID 664510; CID664510; CID-664510; 5-(methylamino)-2-naphthalen-1-yl-1,3-oxazole-4-carbonitrile. Grades: 98%. CAS No. 847163-28-4. Molecular formula: C15H11N3O. Mole weight: 249.27.
ML 354
ML 354 is a selective PAR4 antagonist with IC50 value of 140 nM. Synonyms: ML354; ML-354; ML 354; VU0099704; VU-0099704; VU 0099704; 1-Methyl-5-nitro-3-phenyl-1H-indole-2-methanol. Grades: ≥98% by HPLC. CAS No. 89159-60-4. Molecular formula: C16H14N2O3. Mole weight: 282.29.
ML355
ML355 inhibits PAR-4 induced aggregation and calcium mobilization in human platelets and reduce 12-HETE in β-cells. Synonyms: ML 355; ML-355. Grades: >98%. CAS No. 1532593-30-8. Molecular formula: C21H19N3O4S2. Mole weight: 441.52.
ML-356
ML-356 is a potent and selective inhibitor of the thioesterase domain of fatty acid synthase (FASN-TE). It blocks the biosynthesis of palmitate, the end product of FASN. Synonyms: ML 356; ML356; 2-Ethyl-N-[4-(4-morpholin-4-ylsulfonylphenyl)-1,3-thiazol-2-yl]butanamide. Grades: ≥98%. CAS No. 1808260-45-8. Molecular formula: C19H25N3O4S2. Mole weight: 423.5.
ML364
ML364 is a small molecule, reversible inhibitor of the deubiquitinase USP2, that has an IC50 value of 1.1 μM in a fluorescence-based assay using di-ubiquitin substrates. Consistent with the role of cyclin D1 in DNA damage response, ML364 also caused a decrease in homologous recombination-mediated DNA repair. Synonyms: 2-[(4-Methylphenyl)sulfonylamino]-N-(4-phenyl-1,3-thiazol-2-yl)-4-(trifluoromethyl)benzamide; ML364; ML 364; ML-364. CAS No. 1991986-30-1. Molecular formula: C24H18F3N3O3S2. Mole weight: 517.54.
ML-365
ML-365 is a potent and novel selective small molecule inhibitor of TASK1 with IC50 of 4 nM(thallium influx fluorescent assay) and 16 nM(automated electrophysiology assay). It possesses more than 60-fold selectivity for inhibition of TASK1 over TASK3. It displays little or no inhibition at 30 μM of more distantly related Kir2.1, voltage-gated potassium channel, KQT-like subfamily, member 2 (KCNQ2) and human ether-a go-go-related gene (hERG). It is a useful pharmacological probe for in vitro studies of TASK1 function. It mainly aimed at developing therapeutic intervention in further studies. Uses: Ml365 is a useful pharmacological probe for in vitro studies of task1 function. it mainly aimed at developing therapeutic intervention in further studies. Synonyms: 2-Methoxy-N-(3-(3-methylbenzamido)phenyl)benzamide; ML365; ML-365; ML 365. Grades: >98 %. CAS No. 947914-18-3. Molecular formula: C22H20N2O3. Mole weight: 360.41.
ML398 hydrochloride
ML398 is potent dopamine 4 receptor antagonist with IC50 value of 130 nM and Ki of 36 nM. It exhibits no activity against the other dopamine receptors tested (>20 μM against D1, D2S, D2L, D3, and D5) ML398 shows >100-fold selectivity for the other dopamine receptors. Synonyms: ML398 hydrochloride; ML 398 hydrochloride; ML-398 hydrochloride; (R)-4-((1H-benzo[d]imidazol-2-yl)methyl)-2-phenethylmorpholine hydrochloride. Grades: 98%. CAS No. 1379510-21-0. Molecular formula: C20H24ClN3O. Mole weight: 357.88.
ML 786 dihydrochloride
ML786 dihydrochloride is a Raf kinase inhibitor with IC50 values are 2.1, 2.5 and 4.2 nM for B-RafV600E, C-Raf and wild-type B-Raf respectively. It may be used in novel cancer therapies in the future. Synonyms: MLN786 Dihydrochloride; MLN-786 Dihydrochloride; MLN 786 Dihydrochloride; MLN786 2HCl; MLN-786 2HCl; MLN 786 2HCl; 3-(1-Amino-1-methylethyl)-N-[(2R)-1,2,3,4-tetrahydro-7-oxo-1,8-naphthryridin-4-yl)oxy]-2-naphthalenyl]-5-benzamide dihydrochloride. Grades: ≥98% by HPLC. CAS No. 1237536-18-3. Molecular formula: C29H29F3N4O3.2HCl. Mole weight: 611.48.
ML-7 hydrochloride
ML-7 Hcl is a cell-permeable, potent, reversible, ATP-competitive, and selective inhibitor of myosin light chain kinase (Ki = 300 nM). It also inhibt smooth-muscle myosin light chain kinase, protein kinase C (PKC) and cAMP-dependent protein kinase (PKA). Synonyms: ML-7 HCl; ML-7 hydrochloride; ML-7; ML 7; ML7. Grades: >98%. CAS No. 110448-33-4. Molecular formula: C15H18ClIN2O2S. Mole weight: 452.74.
MLi-2
MLi-2 is a potent, orally available and brain penetrant inhibitor of LRRK2 (IC50 = 0.76 nM) with excellent selectivity that shows >295-fold selectivity for over 300 kinases and a diverse panel of receptors and ion channels. Synonyms: (2R,6S)-2,6-dimethyl-4-[6-[5-(1-methylcyclopropyl)oxy-1H-indazol-3-yl]pyrimidin-4-yl]morpholine; MLi-2; MLi 2; MLi2. CAS No. 1627091-47-7. Molecular formula: C21H25N5O2. Mole weight: 379.46.
MLN0905
MLN0905 is a potent, selective small-molecule PLK1 inhibitor. MLN0905 inhibits cell proliferation in a broad range of human tumor cells including DLBCL cell lines. PLK1 inhibition leads to pharmacodynamic pHisH3 modulation and significant antitumor activity in multiple DLBCL models. These data strongly suggest evaluating PLK1 inhibitors as DLBCL anticancer agents in the clinic. Synonyms: MLN0905; MLN0905; MLN0905. CAS No. 1228960-69-7. Molecular formula: C24H25F3N6S. Mole weight: 486.561.
MLN1117
MLN1117, also known as INK1117, is a PI3Kα inhibitor which could lead to the apoptosis and growth retardation of tumor cells expressed by PI3K&alpha. IC50: 15 nM. Uses: Mln1117 is a pi3kα inhibitor which could lead to the apoptosis and growth retardation of tumor cells expressed by pi3k&alpha. Synonyms: INK1117; INK-1117; INK 1117; MLN1117; MLN 1117; MLN-1117; TAK-117; TAK 117; TAK117; Serabelisib; [6-(2-amino-1,3-benzoxazol-5-yl)imidazo[1,2-a]pyridin-3-yl]-morpholin-4-ylmethanone;Serabelisib. Grades: 98%. CAS No. 1268454-23-4. Molecular formula: C19H17N5O3. Mole weight: 363.37.