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PF-68742
PF-68742 is a new entry inhibitor of CCR5- and CXCR4- tropical strains of human immunodeficiency virus type 1 (HIV-1), targeting a new site on gp41. Synonyms: PF 68742; PF68742. Grades: ≥98% by HPLC. Molecular formula: C28H33FN4O6S. Mole weight: 572.65.
PF 750
PF 750 is a potent, time-dependent, irreversible FAAH inhibitor (IC50 = 16.2 nM) that exhibits no activity at a range of other serine hydrolases. Activity-based profiling of various human and murine tissue proteome samples revealed that PF-750 is highly selective for FAAH relative to other serine hydrolases, showing no discernable off-site activity up to 500 μM. Synonyms: PF-750; PF 750; PF750. N-Phenyl-4-(3-quinolinylmethyl)-1-piperidinecarboxamide. Grades: ≥98% by HPLC. CAS No. 959151-50-9. Molecular formula: C22H23N3O. Mole weight: 345.44.
PF 915275
PF-915275 is a selective and potent and inhibitor of human 11β-hydroxysteroid dehydrogenase type 1(11βHSD1) inhibitor with Ki 2.3 nM. It has good preclinical pharmacokinetic properties. It inhibits the conversion of prednisone to prednisolone in human hepatocytes in vitro and has antidiabetic activity in vivo. It maintains potency in our cellular assay against human 11βHSD1 and is selective against human 11βHSD2 in vitro. It displays only weak affinity for the rodent choline transporter (Ki = 9.6 μM) and the hamster melatonin MT3 receptor (Ki = 9.6 μM) in the Cerep Bioprint screening panel. It has good in vitro pharmacokinetic properties. It has low clearance and high permeability. It has an excellent pharmacokinetic profile characterized by low clearance, long half-life and good oral bioavailability. Uses: Pf-915275 inhibits the conversion of prednisone to prednisolone in human hepatocytes in vitro and has antidiabetic activity in vivo. it has an excellent pharmacokinetic profile characterized by low clearance, long half-life and good oral bioavailability. Synonyms: PF-915275; PF 915275; PF915275; N-(6-Amino-2-pyridinyl)-4'-cyano-[1,1'-biphenyl]-4-sulfonamide;N-(6-aminopyridin-2-yl)-4-(4-cyanophenyl)benzenesulfonamide;[1,1'-Bip;4'-cyanobiphenyl-4-sulfonic acid (6-aminopyridin-2-yl)amide. Grades: >98 %. CAS No. 857290-04-1. Molecular formula: C18H14N4O2S. Mole weight: 350.39.
PF 9184
This active molecular is selective mPGES-1 (microsomal prostaglandin E synthase-1 inhibitor. mPGES-1 is an enzyme induced during the inflammatory response and it is for developing anti-inflammatory drugs. PF-9184 inhibited recombinant human mPGES-1 with IC50 value of 16.5nM. PF-9184 had no effect against COX-1 and COX-2 with more than 6500-fold selectivity. PF-9184 inhibited PGE(2) synthesis with IC50 value in the range of 0.5-5 mM in serum-free cell and human whole blood cultures. Uses: Anti-inflammatory agent. Synonyms: N-(3',4'-Dichloro[1,1'-biphenyl]-4-yl)-4-hydroxy-2H-1,2-benzothiazine-3-carboxamide 1,1-dioxide. Grades: 98%. CAS No. 1221971-47-6. Molecular formula: C21H14Cl2N2O4S. Mole weight: 461.31.
PF 945863
PF 945863, an orally active macrolide antibiotic, is active against multidrug resistant respiratory tract bacterial strains. Synonyms: PF 945863; PF945863; PF-945863; (3aS,4R,7R,9R,10R,11R,13R,15R,15aR)-4-Ethyloctahydro-11-methoxy-3a,7,9,11,13,15-hexamethyl-1-[1-[(1R)-1-(1,8-naphthyridin-4-yl)ethyl]-3-azetidinyl]-10-[[3,4,6-trideoxy-3-(dimethylamino)-β-D-xylo-hexopyranosyl]oxy]-2H-oxacyclotetradecino[4,3-d]oxazole-2,6,8,14(1H,7H,9H)tetrone. Grades: ≥98% by HPLC. CAS No. 893556-85-9. Molecular formula: C44H65N5O10. Mole weight: 824.01.
PF-956980
PF-956980, a close analogue of Tofacitinib, is a JAK3-selective inhibitor used as an anti-inflammatory agent. Besides, some studies showed that PF-956980 strikingly reversed the cytoprotective action of IL-4 on CLL cells. Synonyms: PF-956980; PF 956980; PF956980; Methanone, [(3R,?4R)?-4-methyl-3-(methyl-7H-pyrrolo[2,?3-d]?pyrimidin-4-ylamino)?-1-piperidinyl]?-1-pyrrolidinyl-. CAS No. 1262832-74-5. Molecular formula: C18H26N6O. Mole weight: 342.44.
PF 998425
PF 998425 is a novel, nonsteroidal androgen receptor (AR) antagonist (IC50= 26 nM and 90 nM in AR binding assays and cellular assays respectively) for sebum control and treatment of androgenetic alopecia. It is potent, selective, and active in vivo. PF 998425 exhibits low affinity for progesterone receptor (IC50 > 10 μM). Uses: Androgen receptor antagonists. Synonyms: 4-((1R,2R)-2-Hydroxycyclohexyl)-2(trifluoromethyl)benzonitrile; PF0998425; PF 0998425; PF-0998425. Grades: ≥98% by HPLC. CAS No. 1076225-27-8. Molecular formula: C14H14F3NO. Mole weight: 269.26.
PF-AKT400
PF-AKT400 is an APT competitor inhibitor of AKR kinase. This compound was first described as compound 42 in J. Med. Chem. 2010, 53, 4615-4622 by a group of Pfizer scientists. The paper describes the design and synthesis of novel, ATP-competitive Akt inhibitors from an elaborated 3-aminopyrrolidine scaffold. Key findings include the discovery of an initial lead that was modestly selective and medicinal chemistry optimization of that lead to provide more selective analogues. Analysis of the data suggested that highly lipophilic analogues would likely suffer from poor overall properties. Central to the discussion is the concept of optimization of lipophilic efficiency and the ability to balance overall druglike propeties with the careful control of lipophilicity in the lead series. Discovery of the nonracemic amide series and subsequent modification produced an advanced analogue that performed well in advanced preclinical assays, including xenograft tumor growth inhibition studies, and this analogue was nominated for clinical development. The compound has no official name, has molecule weight 400.43. We temporally call this compound as PF-AKT400. Synonyms: PF-AKT400; PFAKT400; Lig1; Lig-1; Lig 1; PF AKT400; AKT-0286; AKT 0286; AKT0286. CAS No. 1004990-28-6. Molecular formula: C20H22F2N6O. Mole weight: 400.43.
PF-CBP1
PF-CBP1, also known as PF-06670910, is a selective CBP/p300 bromodomain inhibitor (IC50 values are 125 and 363 nM, respectively) with >100-fold selectivity for CBP over BRD4. Also, PF-CBP1 significantly reduces levels of RGS4 mRNA levels in neurons. Synonyms: 4-(2-(5-(3,5-Dimethylisoxazol-4-yl)-2-(4-propoxyphenethyl)-1H-benzo[d]imidazol-1-yl)ethyl)morpholine; PF-CBP1; PF-CBP-1; PF-CBP 1; PF-06670910; PF 06670910; PF06670910.PF-CBP1; PF CBP1; PFCBP1. CAS No. 1962928-21-7. Molecular formula: C29H36N4O3. Mole weight: 488.63.
PF-CBP1 HCl
PF-CBP1, also known as PF-06670910, is an inhibitor of the CBP and p300 bromodomains (IC50s = 125 and 363 nM, respectively) with more than 100-fold selectivity for the bromodomain of CBP over those of BRD4 and a panel of other proteins. Also, PF-CBP1 significantly reduces levels of RGS4 mRNA levels in neurons. Synonyms: 4-(2-(5-(3,5-Dimethylisoxazol-4-yl)-2-(4-propoxyphenethyl)-1H-benzo[d]imidazol-1-yl)ethyl)morpholine hydrochloride; PF-CBP1 HCl; PF-CBP1; hydrochloride; PF-CBP1; PF-CBP-1; PF-CBP 1; PF-06670910; PF 06670910; PF06670910. CAS No. 2070014-93-4. Molecular formula: C29H37ClN4O3. Mole weight: 525.09.
PFI-1
PFI-1 is a potent and highly selective protein interaction Inhibitor, which targets BET bromodomain. PFI-1 that efficiently blocks the interaction of BET BRDs with acetylated histone tails. Co-crystal structures showed that PFI-1 acts as an acetyl-lysine (Kac) mimetic inhibitor efficiently occupying the Kac binding site in BRD4 and BRD2. PFI-1 has antiproliferative effects on leukaemic cell lines and efficiently abrogates their clonogenic growth. Exposure of sensitive cell lines with PFI-1 results in G1 cell cycle arrest, down-regulation of MYC expression as well as induction of apoptosis and induces differentiation of primary leukaemic blasts. Intriguingly, cells exposed to PFI-1 showed significant down-regulation of Aurora B kinase, thus attenuating phosphorylation of the Aurora substrate H3S10 providing an alternative strategy for the specific inhibition of this well established oncology target. Synonyms: PFI1; PFI 1; PFI-1. CAS No. 1403764-72-6. Molecular formula: C16H17N3O4S. Mole weight: 347.39.
PFI-2
PFI-2 is a potent, selective, and cell-active lysine methyltransferase SETD7 inhibitor with Ki (app) and IC50 of 0.33 nM and 2 nM, 1000-fold selectivity over other methyltransferases and other non-epigenetic targets. Synonyms: PFI-2; PFI 2; PFI2. Grades: >98%. CAS No. 1627676-59-8. Molecular formula: C23H25F4N3O3S. Mole weight: 499.52.
PFI-2 hydrochloride
PFI-2 hydrochloride is a potent, cell-permeable inhibitor of SET7/9 (IC50 = 2 nM) and is approximately 1,000-fold selective over a panel of 18 other methyltransferases. Besides, following activation of the Hippo signaling pathway in MCF7 cells it inhibits. Synonyms: PFI-2 hydrochloride; PFI 2 hydrochloride; PFI2 hydrochloride; 8-fluoro-N-[(2R)-1-oxo-1-pyrrolidin-1-yl-3-[3-(trifluoromethyl)phenyl]propan-2-yl]-1,2,3,4-tetrahydroisoquinoline-6-sulfonamide;hydrochloride. CAS No. 1627607-87-7. Molecular formula: C23H26ClF4N3O3S. Mole weight: 535.98.
PFI-4
PFI-4 is a potent and selective BRPF1 bromodomain inhibitor with IC50 of 80 nM. Synonyms: PFI-4; PFI 4; PFI4. Grades: 98%. CAS No. 900305-37-5. Molecular formula: C21H24N4O3. Mole weight: 380.44.
[(pF)Phe4]Nociceptin(1-13)NH2
[(pF)Phe4]Nociceptin(1-13)NH2 is a highly potent and selective nociceptin/orphanin FQ receptor (OP4) agonist peptide (pKi = 10.68; pEC50 = 9.80), with 8000-fold selectivity over δ, κ, and μ opioid receptors. Synonyms: (S, Z)-6-amino-N-((S, Z)-1-(((S, Z)-1-(((S, Z)-1-(((S)-6-amino-1-hydroxy-1-iminohexan-2-yl)imino)-5-guanidino-1-hydroxypentan-2-yl)imino)-1-hydroxypropan-2-yl)imino)-1, 3-dihydroxypropan-2-yl)-2-((Z)-((2S, 3Z, 5S, 6Z, 9Z, 11S, 12Z, 14S, 15Z, 18Z, 21Z, 23S)-23-amino-2-(3-. CAS No. 380620-88-2. Molecular formula: C61H99FN22O15. Mole weight: 1399.6.
PG 01
PG 01 is a cystic fibrosis transmembrane conductance regulator (CFTR) potentiator. PG 01 is effective on G970R although with a significant decrease in potency relative to E193K and ΔF508. Synonyms: PG 01; PG-01; PG01; N-Methyl-N-[2-[[4-(1-Methylethyl)phenyl]amino]-2-1H-indole-3-acetamide. Grades: ≥98% by HPLC. CAS No. 853138-65-5. Molecular formula: C28H29N3O2. Mole weight: 439.55.
PG 01037 dihydrochloride
PG 01037 dihydrochloride is a dopamine D3 receptor antagonist, which is more selective for D3 receptors than other D3 antagonists that are currently available with a D2/D3 selectivity ratio of 867 and a D4/D3 selectivity ratio of 13,000 (Ki values are 0.70, 93.3 and 375 nM for D3, D2 and D4 receptors respectively). Synonyms: N-[(2E)-4-[4-(2,3-Dichlorophenyl)-1-piperazinyl]-2-buten-1-yl]-4-(2-pyridyl)-benzamide dihydrochloride; PG 01037 dihydrochloride; PG 01037 diHCl; PG 01037; PG01037; PG-01037. Grades: ≥98%. CAS No. 675599-62-9. Molecular formula: C26H26Cl2N4O.2HCl. Mole weight: 554.34.
PG-9 maleate, derived from (+)-R-hyoscyamine, is a potent analgesic and nootropic agent, which increases release of acetylcholine. Synonyms: PG-9 maleate; PG 9 maleate; PG9 maleate; Tropanyl 2-(4-bromophenyl)propionate maleate. CAS No. 155649-00-6. Molecular formula: C17H22BrNO2.C4H4O4. Mole weight: 468.34.
pGpA
A STING agonist negative control (pGpA). Synonyms: 3'5'-pGpA sodium salt; 3'3'-cGAMP Control. CAS No. 20137-01-3. Molecular formula: C20H23N10O14P2.3Na. Mole weight: 758.38.
PGPC
PGPC is an oxidized phospholipid formed under conditions of oxidative stress. It is a potent PPARα agonist. Synonyms: 1-Hexadecanoyl-2-glutaroyl-sn-glycero-3-phosphocholine; 1-Palmitoyl-2-glutaryl phosphatidylcholine; 1-Palmitoyl-2-glutaryl-sn-glycero-3-phosphocholine; 2-O-glutaroyl-1-O-palmitoyl-sn-glycero-3-phosphocholine; PC(16:0/5:0(COOH)). Grades: ≥98%. CAS No. 89947-79-5. Molecular formula: C29H56NO10P. Mole weight: 609.73.
PH-064
PH-064 is a sodium channel inhibitor. It is extracted from patent FR 2879460 A1. Synonyms: BIM-46187; BIM 46187; BIM46187; PH-064; PH 064; PH064; (2R)-2-amino-3-[[(2R)-2-amino-3-[(8S)-8-(cyclohexylmethyl)-2-phenyl-6,8-dihydro-5H-imidazo[1,2-a]pyrazin-7-yl]-3-oxopropyl]disulfanyl]-1-[(8S)-8-(cyclohexylmethyl)-2-phenyl-6,8-dihydro-5H-imidazo[1,2-a]pyrazin-7-yl]propan-1-one;Imidazo[1,2-a]pyrazine, 7,7'-[dithiobis[(2R)-2-aMino-1-oxo-3,1-propanediyl]]bis[8-(cyclohexylMethyl)-5,6,7,8-tetrahydro-2-phenyl-, (8S,8'S)- (9CI). Grades: >98 %. CAS No. 892546-37-1. Molecular formula: C44H58N8O2S2. Mole weight: 795.11.
PH11
PH11, an imidazotriazin derivative, has been found to be a FAK inhibitor that could have probable activity in anticancer studies. Synonyms: PH11; PH-11; PH 11; methyl 2-((4-((3,4,5-trimethoxyphenyl)amino)imidazo[1,2-a][1,3,5]triazin-2-yl)amino)benzoate. Grades: 98%. CAS No. 1627843-95-1. Molecular formula: C22H22N6O5. Mole weight: 450.46.
PH-797804
PH-797804 is a diarylpyridinone inhibitor of p38 mitogen-activated protein (MAP) kinase. PH-797804 exhibited exceptionally high specificity against MAP kinases and the related kinases. No cross-reactivity was observed in large panels of kinase screens (selectivity ratio of >500-fold). In cellular assays, PH-797804 demonstrated superior potency and selectivity consistent with the biochemical measurements. PH-797804 has met safety criteria in human phase I studies and is under clinical development for several inflammatory conditions. Understanding the rationale for selectivity at the molecular level helps elucidate the biological function and design of specific p38alpha kinase inhibitors. Synonyms: PH 797804; PH797804; 3-(3-Bromo-4-((2,4-difluorobenzyl)oxy)-6-methyl-2-oxopyridin-1(2H)-yl)-N,4-dimethylbenzamide. CAS No. 586379-66-0. Molecular formula: C22H19BrF2N2O3. Mole weight: 477.30.
PHA 408
PHA 408 is a selective and ATP-competitive IKB kinase-2 (IKK-2) inhibitor (IC50 = 40 nM), which binds IKK-2 tightly with a relatively slow off rate. Synonyms: PHA 408; PHA408; PHA-408; 8-[[5-chloro-2-(4-methylpiperazin-1-yl)pyridine-4-carbonyl]amino]-1-(4-fluorophenyl)-4,5-dihydrobenzo[g]indazole-3-carboxamide. Grades: 99%. CAS No. 503555-55-3. Molecular formula: C29H27ClFN7O2. Mole weight: 560.02.
PHA 543613 dihydrochloride
PHA 543613 dihydrochloride is a potent and selective α7 nicotinic acetylcholine receptor (nAChR) agonist with rapid brain penetration and high oral bioavailability. PHA 543613 is potentially used for the treatment of cognitive deficits in schizophrenia. Uses: Potential treatment of cognitive deficits in schizophrenia. Synonyms: PHA 543613 dihydrochloride; PHA543613 dihydrochloride; PHA-543613 dihydrochloride; N-[(3R)-1-azabicyclo[2.2.2]octan-3-yl]furo[2,3-c]pyridine-5-carboxamide dihydrochloride. Grades: 99%. CAS No. 478148-58-2. Molecular formula: C15H17N3O2.2HCl. Mole weight: 344.24.
PHA 543613 hydrochloride
PHA 543613 is a potent and selective α7 nAChR agonist. It was shown to reduce Aβ-induced cognitive deficits and increase the α7 protein level and subsequent neuron survival. It has been developed as a potential therapeutic agent for cognitive deficits in schizophrenia. Synonyms: N-(3R)-1-Azabicyclo[2.2.2]oct-3-yl-furo[2,3-c]pyridine-5-carboxamide hydrochloride; N-(1-azabicyclo[2.2.2]octan-3-yl)furo[2,3-c]pyridine-5-carboxamide hydrochloride. Grades: ≥98% by HPLC. CAS No. 1586767-92-1. Molecular formula: C15H17N3O2·HCl. Mole weight: 307.78.
PHA 568487
PHA 568487 is an orally active and brain penetrant agonist of the alpha 7 nicotinic acetylcholine receptor (Ki = 44 and 2800 for α7 and 5-HT3 respectively, IC50=> 100 μM for α3β4 and α1β1δγ respectively, and % inhibition is < 1 and 5% for α4β2 and hERG respectively), which was designed to mitigate the bioactivation associated with the core scaffold and subsequently remove associated liabilities with in vivo tolerability. Synonyms: PHA 568487; PHA568487; PHA-568487; N-(3R)-1-Azabicyclo[2.2.2]oct-3-yl-2,3-dihydro-1,4-benzodioxin-6-carboxamide fumarate. Grades: ≥99% by HPLC. CAS No. 527680-57-5. Molecular formula: C16H20N2O3.C4H4O4. Mole weight: 404.41.
PHA665752
PHA665752 is a small-molecule inhibitor of c-Met/HGF/SF signaling c-Met is highly expressed in most tumors from patients with advanced-stage, metastatic NBL. Furthermore, using the NBL cell line SH-EP as a model, PHA665752 was shown to inhibit cMet/HGF/SF signaling in vitro, suggesting c-Met inhibitors may have efficacy for blocking local progression and/or metastatic spread of c-Met-positive NBL in vivo. These are novel findings for this disease and suggest that further studies of agents targeting the c-Met/HGF axis in NBL are warranted. Synonyms: PHA-665752; PHA 665752. Grades: >98%. CAS No. 477575-56-7. Molecular formula: C32H34Cl2N4O4S. Mole weight: 641.608.
PHA-680632
PHA-680632 is a is potent inhibitor of Aurora A, Aurora B and Aurora C with IC50 of 27 nM, 135 nM and 120 nM. PHA-680632 is also the first representative of a new class of Aurora inhibitors with a high potential for further development as an anticancer therapeutic. Synonyms: PHA-680632; PHA 680632; PHA680632. CAS No. 398493-79-3. Molecular formula: C28H35N7O2. Mole weight: 501.62.
PHA-767491
PHA-767491 is a potent, ATP-competitive dual cdc7/cdk9 inhibitor (IC50 values are 10 and 34 nM respectively) that prevents initiation of DNA replication. Synonyms: PHA-767491; PHA767491; PHA 767491. CAS No. 845714-00-3. Molecular formula: C12H11N3O. Mole weight: 213.24.
PHA-767491 hydrochloride
PHA-767491 hydrochloride is a potent, ATP-competitive dual Cdc7/Cdk9 inhibitor, which prevents initiation of DNA replication. It inhibits cell proliferation in a variety of human cell lines and induces apoptosis in a p53-independent manner in vivo. It also inhibits mitogen-activated protein kinase-activated protein kinase-2 (MK2). Synonyms: CAY-10572 hydrochloride; PHA-767491 hydrochloride; CAY 10572 hydrochloride; PHA 767491 hydrochloride; CAY10572 hydrochloride; PHA767491 hydrochloride. Grades: >98%. CAS No. 942425-68-5. Molecular formula: C12H12ClN3O. Mole weight: 249.7.
PHA-793887
PHA-793887 is an inhibitor of multiple cyclin dependent kinases (CDK) with activity against CDK2, CDK1 and CDK4. Although toxicity was acceptable at initial dose levels, PHA-793887 was poorly tolerated at doses ≥44 mg/m2. The most frequent events across all dose levels were gastrointestinal or nervous system events. PHA-793887 induces severe, dose-related hepatic toxicity, which was not predicted by pre-clinical models and currently precludes its further clinical development. Synonyms: PHA 793887; PHA793887. Grades: >98%. CAS No. 718630-59-2. Molecular formula: C19H31N5O2. Mole weight: 361.48.
Phaclofen
Phaclofen, a phosphonic acid derivative of Baclofen, is a selective GABAB antagonist. Uses: Gaba antagonists. Synonyms: (RS)-3-Amino-2-(4-chlorophenyl)propylphosphonic acid. Grades: ≥97% by HPLC. CAS No. 114012-12-3. Molecular formula: C9H13ClNO3P. Mole weight: 249.63.
[Phe1Ψ(CH2-NH)Gly2]Nociceptin(1-13)NH2
[Phe1Ψ(CH2-NH)Gly2]Nociceptin(1-13)NH2 is the first selective antagonist to prevent the binding of the endogenous ligand orphanin FQ?/Nociceptin (OFQ?/N) at the orphan opioid-like receptor, demonstrated both in vitro and in vivo. It is selective, competitive antagonism at the nociceptin receptor has also been reported (pA2 = 7.02 and 6.75 in the guinea pig ileum and mouse vas deferens respectively). Synonyms: (2S) -6-amino-2- [ [ (2S) -2- [ [ (2S) -2- [ [ (2S) -2- [ [ (2S) -6-amino-2- [ [ (2S) -2- [ [ (2S) -2- [ [2- [ [ (2S, 3R) -2- [ [ (2S) -2- [ [2- [ [2- [ [ (2S) -2-amino-3-phenylpropyl] amino] acetyl] amino] acetyl] amino] -3-phenylpropanoyl] amino] -3-hydroxybutanoyl] amino] acetyl] amino] propanoyl] amino] -5- (diaminomethylideneamino) pentanoyl] amino] hexanoyl] amino] -3-hydroxypropanoyl] amino] propanoyl] amino] -5- (diaminomethylideneamino) pentanoyl] amino] hexanamide; N-[(2S)-2-Amino-3-phenylpropyl]glycylglycyl-L-phenylalanyl-L-threonylglycyl-L-alanyl-L-arginyl-L-lysyl-L-seryl-L-alanyl-L-arginyl-L-lysinamide; N-[(2S)-2-Amino-3-phenylpropyl]-13-L-lysinamide-2-13-orphanin FQ (swine). CAS No. 213130-17-7. Molecular formula: C61H102N22O14. Mole weight: 1367.6.
[Phe8Y(CH-NH)Arg9]-Bradykinin
[Phe8Y(CH-NH)Arg9]-Bradykinin is a selective bradykinin B2 receptor agonist with 5-fold potency against bradykinin in vivo. It is resistant to carboxypeptidase cleavage. Uses: Hypotensive agent. Synonyms: Ppcna-BK; 8-Phe-9-psi-CH2NH-arg-bradykinin. CAS No. 118122-39-7. Molecular formula: C50H75N15O10. Mole weight: 1046.23.
Phenacetin
Phenacetin is a non-opioid analgesic without anti-inflammatory properties. It is a pain-relieving and fever-reducing drug and was withdrawn from the Canadian market in June 1973 due to concerns regarding nephropathy. Phenacetin has been linked to renal papillary necrosis in human beings. Synonyms: p-Acetophenetidide; 4-(Acetylamino)phenetole; 4-Ethoxy-1-acetylaminobenzene; 4-Ethoxyacetanilide; 4'-Ethoxyacetanilide; Aceto-4-phenetidine; Acetophenetidine; Acetophenetin; Acetphenetidin; Fenidina; Fenina; Kalmin; N-Acetyl-4-ethoxyaniline; N-Acetyl-p-ethoxyaniline; N-Acetyl-p-phenetidine; NSC 7651; Pertonal; Phenacetine; Phenidin; Phenin; p-Ethoxyacetanilide. Grades: 97 %. CAS No. 62-44-2. Molecular formula: C10H13NO2. Mole weight: 179.22.
Phenelzine
Phenelzine is hydrazine compound as a a non-selective and irreversible monoamine oxidase inhibitor (MAOI). Uses: A non-selective and irreversible monoamine oxidase inhibitor. Synonyms: 2-phenylethylhydrazine; 1-(2-Phenylethyl)hydrazine. Grades: ≥95%. CAS No. 51-71-8. Molecular formula: C8H12N2. Mole weight: 136.2.
Phenethipylone
Phenethipylone is a selective estrogen receptor modulator. It is a raloxifene analog. Uses: Either first generation because they demonstrate estrogen agonist properties in the endometrium or second generation based on their patterns of tissue specificity. (horm res 1997;48:155-63) (see all compounds cselective estrogen receptor modulators. Synonyms: [6-Hydroxy-2- (4-hydroxyphenyl) benzo[b]thiophen-3-yl][4-[2- (1-pyrrolidinyl) ethoxy]phenyl]methanone; Methanone, (6-hydroxy-2-(4-hydroxyphenyl)benzo(B)thien-3-yl)(4-(2-(1-pyrrolidinyl)ethoxy)phenyl)-; LY 117018; LY117018; LY-117018. Grades: 98%. CAS No. 63676-25-5. Molecular formula: C27H25NO4S. Mole weight: 459.56.
Phenibut
Phenibut is an analog of GABA that acts as a GABAB receptor agonist. It is marketed as a central nervous system depressant used to treat anxiety. Synonyms: Aminophenylbutyric acid; Fenibut; Fenigam; Phenigam; Phenybut; PhGABA; β-Phenyl-γ-aminobutyric acid; β-Phenyl-GABA; 4-Amino-3-phenylbutanoic acid. CAS No. 1078-21-3. Molecular formula: C10H13NO2. Mole weight: 179.22.
Phenoxybenzamine Hydrochloride
Phenoxybenzamine HCl is a non-specific, irreversible alpha antagonist with an IC50 of 550 nM. Uses: Adrenergic alpha-antagonists. Synonyms: Phenoxybenzamine hydrochloride; 63-92-3; Phenoxybenzamine Hcl; DibenzylineN-benzyl-N-(2-chloroethyl)-1-phenoxypropan-2-amine hydrochloride. Grades: >98%. CAS No. 63-92-3. Molecular formula: C18H22ClNO·HCl. Mole weight: 340.3.
Phenserine
Phenserine, an analog of physostigmine, is an acetylcholinesterase (AChE) inhibitor (IC50= 24 nM) potentially for the treatment of Alzheimer Disease (AD). Synonyms: (3aS,8aR)-1,2,3,3a,8,8a-Hexahydro-1,3a,8-trimethylpyrrolo[2,3-b]indol-5-ol 5-(N-phenylcarbamate); (-)-Eseroline phenylcarbamate; (-)-N-Phenylcarbamoyleseroline; (-)-Phenserine. Grades: ≥98% by HPLC. CAS No. 101246-66-6. Molecular formula: C20H23N3O2. Mole weight: 337.42.
Phenylethanolamine A
Phenylethanolamine A is a novel beta-agonist naturally occuring in animal species. Synonyms: 1-(4-Methoxyphenyl)-2-[1-methyl-3-(4-nitrophenyl)-propylamino]-ethanol. CAS No. 1346746-81-3. Molecular formula: C19H24N2O4. Mole weight: 344.4.
Phenylglyoxal hydrate
Phenylglyoxal is a potent inhibitor of mitochondrial aldehyde dehydrogenase. It reacts with arginine residues in purified Hageman factor (HF, Factor XII) and causes inhibition of its coagulant properties. Synonyms: 2,2-Dihydroxy-1-phenylethanone. CAS No. 1075-06-5. Molecular formula: C8H6O2. Mole weight: 134.13.
Phenytoin Sodium
Phenytoin Sodium is a potent multi-channel blocker, which blocks Na+, K+ and Ca 2+ channels and selectively blocks persistent INaP over shorter INaP actions. Grades: >98%. CAS No. 630-93-3. Molecular formula: C15H11N2NaO2. Mole weight: 274.25.
Philanthotoxin 74
Philanthotoxin 74, also called as PhTx-74, is a synthetic analog of the naturally-occurring wasp venom toxin philanthotoxin-4,3,3. Philanthotoxin 74 is an AMPA receptor antagonist, and a non-selective homomeric GluR3 and GluR1 receptor antagonist (IC50= 263 and 296 nM respectively). Synonyms: (S)-N-[7-[(4-Aminobutyl)amino]heptyl]-4-hydroxy-α-[(1-oxobutyl)amino]benzenepropanamide dihydrochloride; Philanthotoxin-74 HCl; Philanthotoxin74; Philanthotoxin 74; PhTx-74; PhTx 74; PhTx74. Grades: ≥98% by HPLC. CAS No. 1227301-51-0. Molecular formula: C24H42N4O3.2HCl. Mole weight: 507.54.
PHM 27 (human)
PHM 27 (human) is an endogenous peptide product of human prepro-VIP and analog of porcine PHI-27. It selectively activated the hCTr; no activity was observed at the PTH1, CRF1, or GLP1 receptors. PHM-27 was a potent agonist at the hCTr, with similar efficacy as human calcitonin, and a potency of 11 nM. Synonyms: PHM 27 (human); PHM27 (human); PHM-27 (human); HADGVFTSDFSKLLGQLSAKKYLESLM; Peptide histidine methionine 27 (human); Human PHI 27; His-Ala-Asp-Gly-Val-Phe-Thr-Ser-Asp-Phe-Ser-Lys-Leu-Leu-Gly-Gln-Leu-Ser-Ala-Lys-Lys-Tyr-Leu-Glu-Ser-Leu-Met-NH2. CAS No. 118025-43-7. Molecular formula: C135H214N34O40S. Mole weight: 2985.44.
(-)-PHNO hydrochloride
(-)-PHNO hydrochloride is a potent and selective dopamine D2 agonist. Synonyms: Ent-Naxagolide Hydrochloride; (-)-Propyl-9-hydroxynaphthoxazine Hydrochloride; (4aS-trans)-3,4,4a,5,6,10b-Hexahydro-4-propyl-2H-naphth[1,2-b]-1,4-oxazin-9-ol Hydrochloride. Grades: 98%. CAS No. 100935-99-7. Molecular formula: C15H21NO2.HCl. Mole weight: 283.79.
(+)-PHNO hydrochloride
(+)-PHNO hydrochloride is a potent and selective dopamine D2 agonist. Synonyms: (4aR-trans)-3,4,4a,5,6,10b-Hexahydro-4-propyl-2H-naphth[1,2-b]-1,4-oxazin-9-ol Hydrochloride; (+)-Propyl-9-hydroxynaphthoxazine Hydrochloride; L 647339; MK 458; Dopazinol Hydrochloride; Nazagolide HCl. Grades: 99%. CAS No. 99705-65-4. Molecular formula: C15H21NO2.HCl. Mole weight: 283.79.
PHOP
PHOP is a potent FAAH inhibitor with Ki values of 0.094 nM and 0.2 nM for the human and rat enzymes, respectively. Synonyms: CAY10402; Phenyl hexanoyl oxazolopyridine; 1-(oxazolo[4,5-b]pyridin-2-yl)-6-phenylhexan-1-one. Grades: ≥98%. CAS No. 288862-83-9. Molecular formula: C18H18N2O2. Mole weight: 294.4.
Phorbol
Phorbol, derived from the roots of Euphorbia pekinensis Rupr., as a tumor promoter it is able to activate protein kinase C. Synonyms: 4β, 9α, 12β, 13α, 20-Pentahydroxytiglia-1, 6-dien-3-one; 4-alpha-phorbol; 4alpha-phorbol; beta-phorbol; isophorbol; phorbol; phorbol, (1aR-(1aalpha, 1bbeta, 4aalpha, 7aalpha, 7balpha, 8alpha, 9beta, 9bbeta))-isomer. CAS No. 17673-25-5. Molecular formula: C20H28O6. Mole weight: 364.4.
Phorbol 12,13-dibutyrate
Phorbol 12,13-dibutyrate, a protein kinase C activator, stimulates the phosphorylation of Na+,K+- ATPase, thereby inhibiting its activity. Uses: Carcinogens. Synonyms: (1aR,1bS,4aR,7aS,7bS,8R,9R,9aS)-1a,1b,4,4a,5,7a,7b,8,9,9a-Decahydro-4a,7b-dihydroxy-3-(hydroxymethyl)-1,1,6,8-tetramethyl-5-oxo-1H-cyclopropa[3,4]benz[1,2-e]azulen-9,9a-diyl butanoic acid ester; 12,13-Dibutyrate, Phorbol; Phorbol 12,13 Dibutyrate; Phorbol 12,13-Dibutyrate; Phorbol-12,13-Dibutyrate. CAS No. 37558-16-0. Molecular formula: C28H40O8. Mole weight: 504.61.
Phospho-Glycogen Synthase Peptide-2 (substrate)
Phospho-Glycogen Synthase Peptide-2 (substrate) is a synthetic peptide suitable as a substrate for glycogen synthase kinase-3 (GSK-3). Synonyms: YRRAAVPPSPSLSRHSSPHQSEDEEE. CAS No. 851366-97-7. Molecular formula: C123H191N40O48P. Mole weight: 3029.
PHP 501 trifluoroacetate
PHP 501 trifluoroacetate is potent GABAA antagonist (Ki = 0.0028 μM at rat GABAA receptors; IC50 = 0.024 μM at human α1β2γ2 GABAA-expressing tsA201 cells), without disrupting hGAT-1, hGAT-2, hGAT-3 or hBGT-1 GABA transporters. Synonyms: PHP 501 trifluoroacetate; PHP501 trifluoroacetate; PHP-501 trifluoroacetate; 4-(5-[1,1'-Biphenyl]-3-yl-1-hydroxy-1H-pyrazol-4-yl)piperidine trifluoroacetate. Grades: ≥98% by HPLC. CAS No. 1236105-75-1. Molecular formula: C20H21N3O.CF3CO2H. Mole weight: 433.42.
PHT-427
PHT-427 is an AKT inhibitor that inhibits AKT and PDPK1 at low micromolar concentrations in numerous cancer cell lines and exhibits good oral anti-tumor activity in mouse xenograft models. PHT-427 reduces the phosphorylation of AKT and PDPK1. Following the administration of a single oral dose of PHT-427 to mice bearing BxPC-3 human pancreatic tumor xenografts, PHT-427 inhibited the phosphorylation of both Akt and PDPK1 as well as downstream targets maximally at 8-12 h after administration corresponding to its peak plasma concentration, with PDPK1 inhibition extending to 24 hr. Anti-tumor activity was observed in a number of human tumor xenografts with in some cases complete cessation of tumor growth during administration of the compound and some tumor regressions observed. Mutational profiles indicate that EGFR and PIK3CA activiating mutations provide greatest sensitivity to PHT-427. Pre-clinical development of PHT-427 continues. Synonyms: PHT-427; PHT427; PHT 427. CAS No. 1191951-57-1. Molecular formula: C20H31N3O2S2. Mole weight: 409.60904.
Phthalazinone pyrazole
Phthalazinone pyrazole is a potent, selective and orally bioavailable inhibitor of Aurora-A kinase. It was shown to arrest mitosis and inhibit tumor growth. Synonyms: 1(2H)-Phthalazinone, 4-[(5-methyl-1H-pyrazol-3-yl)amino]-2-phenyl-; 4-[(5-Methyl-1H-pyrazol-3-yl)amino]-2-phenyl-1(2H)-phthalazinone; 4-[(5-Methyl-1H-pyrazol-3-yl)amino]-2-phenyl-2H-phthalazin-1-one. Grades: ≥98%. CAS No. 880487-62-7. Molecular formula: C18H15N5O. Mole weight: 317.35.
Phthalylsulfacetamide
Phthalylsulfacetamide, a sulfanilamide derivative, is a predrug of sulfacetamide and could be used as an antibacterial agent. Uses: Phthalylsulfacetamide is a predrug of sulfacetamide and could be used as an antibacterial agent. Synonyms: LABOTEST-BB LT00438470;4'-(ACETYLSULFAMOYL)PHTHALANILIC ACID; 2- ([[4- ([ACETYLAMINO]SULFONYL) PHENYL]AMINO]CARBONYL) BENZOIC ACID;N-(4-ACETYLSULFAMOYL-PHENYL)-PHTHALAMIC ACID; N1-ACETYL-N4-PHTHALYLSULFANILAMIDE; PHTHALYLSULFACETAMIDE; 2-((4-[(Acetylamino)sulfon. Grades: 98%. CAS No. 131-69-1. Molecular formula: C16H14N2O6S. Mole weight: 362.36.
PI-103 is a potent, cell-permeable, ATP-competitive inhibitor of phosphatidylinositol 3-kinase (PI3K) family members with selectivity toward DNA-PK, PI3K (p110α), and mTOR. Synonyms: 3-(4-morpholinopyrido[3',2':4,5]furo[3,2-d]pyrimidin-2-yl)phenol; PI103; PI-103; PI 103. Grades: >98%. CAS No. 371935-74-9. Molecular formula: C19H16N4O3. Mole weight: 348.362.
PI-103 Hydrochloride
A selective class I PI3K inhibitor; it inhibits PI3K p110 isoforms, mTOC1 and also DNA-PK; a valuable tool compound. Synonyms: PI 103 hydrochloride; PI103 hydrochloride. Grades: >98%. CAS No. 371935-79-4. Molecular formula: C19H17ClN4O3. Mole weight: 384.82.
PI-1840
PI-1840 potently inhibits proteasomal CT-L activity with IC50 of 0.37 μM in intact human MDA-MB-468 cancer cells, and inhibits proliferation/survival of human MDA-MB-468 cells. Synonyms: PI-1840; PI 1840; PI1840. Grades: >98%. CAS No. 1401223-22-0. Molecular formula: C22H26N4O3. Mole weight: 394.47.
PI3Kα inhibitor 1
PI3Kα inhibitor 1 is an inhibitor of PI3Kα as well as HDAC and probably have antineoplastic activity. IC50: <0.1 μM. Uses: Pi3kα inhibitor 1 is an inhibitor of pi3kα as well as hdac and probably have antineoplastic activity. Synonyms: PI3Kα inhibitor 1; MDK9521; MDK-9521; MDK 9521; PI3Kα-IN-243; 5-Pyrimidinecarboxamide, N-hydroxy-2-[methyl[[2-[6-(methylamino)-3-pyridinyl]-4-(4-morpholinyl)thieno[3,2-d]pyrimidin-6-yl]methyl]amino]-. Grades: 98%. CAS No. 1235449-52-1. Molecular formula: C23H25N9O3S. Mole weight: 507.57.
PI3Kα/mTOR-IN-1
PI3Kα/mTOR-IN-1 is a potent dual inhibitor of PI3Kα/mTOR (Kis= 10.6 nM and 12.5 nM for mTOR and PI3Kα, respectively). Synonyms: Pyrido[2,3-d]pyrimidin-7(8H)-one, 2-amino-8-cyclopentyl-4-methyl-6-(1H-pyrazol-4-yl)-. CAS No. 1013098-90-2. Molecular formula: C16H18N6O. Mole weight: 310.35.
PI3Kδ-IN-2
PI3Kδ-IN-2 is a potent and selective inhibitor ofPI3Kδ (IC50= 6.4 M). CAS No. 1702816-75-8. Molecular formula: C28H37FN6O5S. Mole weight: 588.69.
PI3Kδ-IN-7n
PI3Kδ-IN-7n is a potent and highly selective inhibitor of PI3Kδ with IC50 value of 0.9 nM. Synonyms: Selective PI3Kδ Inhibitor 1. CAS No. 2088525-31-7. Molecular formula: C23H20FN7O. Mole weight: 429.45.
PI3k(delta) inhibitor 1
PI3kδ inhibitor 1 is a potent and selective inhibitor of isoform of PI3Kδ; useful for treating disorders mediated by lipid kinases such as inflammation, immunol disorders, and cancer. Synonyms: 2-[1-[[2-(5-Fluoro-1H-indol-4-yl)-4-(morpholin-4-yl)pyrido[3,2-d]pyrimidin-6-yl]methyl]piperidin-4-yl]propan-2-ol. Grades: >98%. CAS No. 1332075-63-4. Molecular formula: C28H33FN6O2. Mole weight: 504.6.
PI3-Kinase α Inhibitor 2
PI3-Kinase α (PI3Kα) inhibitor 2 is a potent inhibitor of PI3K p110α (IC50 = 2 nM) with selectivity for p110α over p110β, p110γ, and PI3K C2β (IC50s = 16, 660, and 220 nM, respectively). Synonyms: PI3Kα Inhibitor 2; Phosphatidylinositol 3-Kinase α Inhibitor 2; Compound 15e; 3-(4-morpholin-4-ylthieno[3,2-d]pyrimidin-2-yl)phenol. Grades: ≥98%. CAS No. 371943-05-4. Molecular formula: C16H15N3O2S. Mole weight: 313.4.
PI3-Kinase α Inhibitor 2 hydrochloride
PI3-Kinase α (PI3Kα) inhibitor 2 is a potent inhibitor of PI3K p110α (IC50 = 2 nM) with selectivity for p110α over p110β, p110γ, and PI3K C2β (IC50s = 16, 660, and 220 nM, respectively). Synonyms: Phosphatidylinositol 3-Kinase α Inhibitor 2; PI3Kα Inhibitor 2; 3-(4-Morpholinothieno[3,2-d]pyrimidin-2-yl)phenol hydrochloride. Grades: ≥98%. CAS No. 1188890-32-5. Molecular formula: C16H15N3O2S·2HCl. Mole weight: 386.3.
PI3Ky inhibitor 1
PI3Ky inhibitor 1 is a potent PI3Ky inhibitor. Synonyms: 1172118-03-4; PI3Kgamma inhibitor 1; CHEMBL2216897N-(6-(4-Amino-1-((8-methyl-1-oxo-2-(o-tolyl)-1,2-dihydroisoquinolin-3-yl)-methyl)-1H-pyrazolo[3,4-d]pyrimidin-3-yl)benzo[d]thiazol-2-yl)acetamide; N-[6-[4-amino-1-[[8-methyl-2-(2-methylphenyl)-1-oxoisoquinolin-3-yl]methyl]pyrazolo[3,4-d]pyrimidin-3-yl]-1,3-benzothiazol-2-yl]acetamide. Grades: >98%. CAS No. 1172118-03-4. Molecular formula: C32H26N8O2S. Mole weight: 586.67.
PI 828
PI 828 is a cell permeable 4'-amino derivative which inhibits the p110α, p110β, p110δ, and p110γ subunits of PI 3-kinase. PI-828 is a potent inhibitor of phosphatidylinositol 3-kinase (PI3K; IC50s = 9.8, 183, 227, and 1,967 nM for p110β, p110α, p110δ, and p110γ, respectively) that displays higher potency than LY 294002. Synonyms: LY294002,4'-NH2; PI-828; PI 828; PI828. 2-(4-Morpholinyl)-8-(4-aminopheny)l-4H-1-benzopyran-4-one. Grades: ≥99% by HPLC. CAS No. 942289-87-4. Molecular formula: C19H18N2O3. Mole weight: 322.36.
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