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VU 0155041
VU 0155041 is a potent positive allosteric modulator at mGlu4 receptors (EC50 = 798 and 693 nM at human and rat mGlu4 receptors, respectively). VU 0155041 displays no activity for 67 G protein-coupled receptors, ion channels, and transporters, and lacks antagonist activity at NMDA receptors in striatal medium spiny neurons at a concentration of 10 μM. VU 0155041 is active in in vivo models of Parkinson's disease following i.c.v. administration. Synonyms: VU0155041, VU 0155041, VU-0155041; cis-2-[[ (3, 5-Dichlorophenyl) amino]carbonyl]cyclohexanecarboxylic acid; (1R,2S)-2-[(3,5-dichlorophenyl)carbamoyl]cyclohexane-1-carboxylic acid. Grades: ≥99% by HPLC. CAS No. 1093757-42-6. Molecular formula: C14H15Cl2NO3. Mole weight: 316.18.
VU 0155041 sodium salt
VU 0155041 sodium salt is a potent positive allosteric modulator at mGlu4 receptors (EC50 = 798 and 693 nM at human and rat mGlu4 receptors, respectively). VU 0155041 displays no activity for 67 G protein-coupled receptors, ion channels, and transporters, and lacks antagonist activity at NMDA receptors in striatal medium spiny neurons at a concentration of 10 μM. VU 0155041 is active in in vivo models of Parkinson's disease following i.c.v. administration. Synonyms: VU 0155041 sodium salt; VU0155041 sodium salt; VU-0155041 sodium salt; cis-2-[[ (3, 5-Dichlorophenyl) amino]carbonyl]cyclohexanecarboxylic acid sodium salt. Grades: ≥98% by HPLC. CAS No. 1259372-69-4. Molecular formula: C14H14Cl2NNaO3. Mole weight: 338.16.
VU 0155069
VU 0155069 is a potent and selective phospholipase D1 (PLD1) inhibitor (IC50 = 46 and 933 nM for PLD1 and PLD2, respectively). VU 0155069 has been shown to inhibit migration of human and mouse breast cancer cell lines in transwell assays. Synonyms: VU-0155069; VU 0155069; VU0155069; N-[(1S)-2-[4-(5-Chloro-2,3-dihydro-2-oxo-1H-benzimidazol-1-yl)-1-piperidinyl]-1-methylethyl-2-naphthalenecarboxamide. Grades: ≥98% by HPLC. CAS No. 1130067-06-9. Molecular formula: C26H27ClN4O2. Mole weight: 462.98.
VU 0238429
VU 0238429 is a selective positive allosteric modulator of M5 muscarinic acetylcholine receptor (EC50 = 1.16, >30 and >30 μM at M5, M1 and M3 receptors, respectively) with no activity at M2 and M4 receptors. Synonyms: VU0238429, VU 0238429, VU-0238429; 1-(4-Methoxybenzyl)-5-trifluoromethoxyisatin; 1-[(4-methoxyphenyl)methyl]-5-(trifluoromethoxy)indole-2,3-dione. Grades: ≥99% by HPLC. CAS No. 1160247-92-6. Molecular formula: C17H12F3NO4. Mole weight: 351.28.
VU0238441
VU0238441 is a pan muscarinic acetylcholine receptor (mAChR) positive allosteric modulator (PAM) with EC50s of 3.2 μM, 2.8 μM, 2.2 μM, 2.1 μM, >10 μM for M1, M2, M3, M5 and M4, respectively. Synonyms: 1H-Indole-2,3-dione, 7-chloro-1-[[4-(trifluoromethyl)phenyl]methyl]-. Grades: 98%. CAS No. 85511-68-8. Molecular formula: C16H9ClF3NO2. Mole weight: 339.69.
VU-0240551
VU 0240551 is a small-molecule inhibitor of neuronal K-Cl cotransporter(KCC2) with IC50 value of 560nM, which is a potassium-chloride exchanger expressed specifically in neurons. It also inhibits hERG and L-type Ca2+ channels. It is primarily responsible for maintaining intracellular Cl- concentrations including regulating an excess or lack of ions following periods of under or overstimulation, as well as general dendritic development. It was discovered in a high-throughput screen, followed by directed medicinal chemistry. It is selective for KCC2 and shows minimal effect on NKCC1. It binds competitively to the K+ site and binds noncompetitively to the Cl- site. It is the only small molecule with specificity for a KCC family member. It significantly inhibits KCC2-mediated K+ uptake at concentration of 10μM. It is also found to inhibit KCC3 in the micromolar range. It exerts significant effects on Adenosine A1 and A3 receptors, L- type Ca2+ channel and K+ channel hERG when treated with some other GPCRs, ion channels and transporters. Uses: Vu 0240551 is primarily responsible for maintaining intracellular cl- concentrations including regulating an excess or lack of ions following periods of under or overstimulation, as well as general dendritic development. Synonyms: VU0240551, VU 0240551, VU- 0240551; N-(4-Methyl-2-thiazolyl)-2-[(6-phenyl-3-pyridazinyl)thio]acetamide;VU 0240551. Grades: >99 %. CAS No. 893990-34-6. Molecular formula: C16H14N4OS2. Mole weight: 342.43.
VU 0255035
VU 0255035 is a highly selective M1 muscarinic acetylcholine receptor antagonist (Ki = 14.87 nM) with 75-fold greater selectivity for the M1 orthosteric site over the other receptor subtypes. VU 0255035 has been shown to reduce pilocarpine-induced seizures in mice. Synonyms: VU0255035, VU 0255035, VU-0255035; N-[3-Oxo-3-[4-(4-pyridinyl)-1-piperazinyl]propyl]-2,1,3-benzothiadiazole-4-sulfonamide. Grades: ≥99% by HPLC. CAS No. 1135243-19-4. Molecular formula: C18H20N6O3S2. Mole weight: 432.52.
VU 0285683
VU 0285683 is a negative allosteric modulator of mGlu5 receptors with high affinity for the MPEP binding site. VU 0285683 exhibits anxiolytic activity in rodent models of anxiety. Synonyms: VU0285683, VU 0285683, VU-0285683; 3-Fluoro-5-[3-(2-pyridinyl)-1,2,4-oxadiazol-5-yl]-benzonitrile. Grades: ≥98% by HPLC. CAS No. 327056-22-4. Molecular formula: C14H7FN4O. Mole weight: 266.23.
VU 0357121
VU0357121 is a novel positive allosteric modulator (PAM) of mGlu5 with EC50 of 33 nM, is inactive or very weakly antagonizing at other mGlu receptor subtypes. Synonyms: VU-0357121, VU0357121, VU 0357121. Grades: >98%. CAS No. 433967-28-3. Molecular formula: C17H17F2NO2. Mole weight: 305.32.
VU0359595
VU0359595 is an inhibitor of Phospholipase D1 (PLD1) (IC50 = 3.7 nM) exhibiting >1,700-fold selectivity for PLD1 over PLD2 (IC50 = 6.4 μM). It may function via interacting with an allosteric site of PLD. Synonyms: CID-53361951; ML-270; (1R,2R)-N-([S]-1-{4-[5-bromo-2-oxo-2,3-dihydro-1H-benzo(d)imidazol-1-yl]piperidin-1-yl}propan-2-yl)-2-phenylcyclopropanecarboxamide. Grades: ≥95%. CAS No. 1246303-14-9. Molecular formula: C25H29BrN4O2. Mole weight: 497.43.
VU 0360172 hydrochloride
VU 0360172 hydrochloride is a positive allosteric modulator of mGlu5 receptors (EC50 = 16 nM; Ki = 195 nM) with potential antipsychotic-like activity. VU 0360172 has no significant activity at mGlu1, mGlu2 or mGlu4 receptors. VU 0360172 has been shown to decrease spontaneous spike and wave discharges without affecting motor behavior in a rat model of absence epilepsy. Synonyms: VU 0360172 hydrochloride; VU0360172 hydrochloride; VU-0360172 hydrochloride; N-Cyclobutyl-6-[2-(3-fluorophenyl)ethynyl]-3-pyridinecarboxamide hydrochloride. Grades: ≥98% by HPLC. CAS No. 1309976-62-2. Molecular formula: C18H15FN2O.HCl. Mole weight: 330.78.
VU 0360223
VU 0360223 is a potent mGlu5 negative allosteric modulator (IC50 = 61 nM) that has no activity at mGlu1-4 and mGlu7-8. Synonyms: VU 0360223; VU0360223; VU-0360223; 3-Fluoro-5-(2-methyl-5-benzothiazolyl)-benzonitrile. Grades: ≥99% by HPLC. CAS No. 1274859-33-4. Molecular formula: C15H9FN2S. Mole weight: 268.31.
VU 0361737
VU 0361737 is a selective positive allosteric modulator (PAM) for mGlu4 receptor with EC50 of 240 nM and 110 nM at human and rat receptors, respectively, displaying weak activity at mGlu5 and mGlu8 receptors, and being inactive at mGlu1, mGlu2, mGlu3, mGlu6 and mGlu7 receptors. Synonyms: VU 0361737, VU-0361737, VU0361737. CAS No. 1161205-04-4. Molecular formula: C13H11ClN2O2. Mole weight: 262.693.
VU 0364439
VU 0364439 is a mGlu4 positive allosteric modulator (PAM), with EC50 of 19.8 nM. Synonyms: VU0364439, VU-0364439, VU 0364439. CAS No. 1246086-78-1. Molecular formula: C18H13Cl2N3O3S. Mole weight: 422.28.
VU0364572 trifluoroacetate salt
VU0364572 is an allosteric agonist of the muscarinic acetylcholine receptor 1 (M1) with EC50 value of 0.2 mM. It induces increases in Ca2+ mobilization and ERK1/2 phosphorylation in CHO cells transfected with the human M1 receptor, but exhibits no effect on β-arrestin recruitment. Synonyms: VU0364572 TFA salt; ethyl 4-[(3R)-3-[(2-methylbenzoyl)amino]piperidin-1-yl]piperidine-1-carboxylate;2,2,2-trifluoroacetic acid. Grades: ≥98%. CAS No. 1240514-89-9. Molecular formula: C21H31N3O3·CF3COOH. Mole weight: 487.5.
VU 0364739 hydrochloride
VU 0364739 hydrochloride is a potent and selective phospholipase D2 (PLD2) inhibitor (IC50 = 20 nM), displaying 75-fold selectivity over PLD1 (IC50 = 1500 nM). Synonyms: VU0364739; VU-0364739; VU 0364739; ML-271; ML271, ML 271; VU0364739 HCl; VU0364739 hydrochloride; N-[2-[1-(3-Fluorophenyl)-4-oxo-1,3,8-triazaspiro[4.5]dec-8-yl]ethyl]-2-naphthalenecarboxamide. Grades: ≥98% by HPLC. CAS No. 1244640-48-9. Molecular formula: C26H27FN4O2.HCl. Mole weight: 482.98.
VU 0365114
VU 0365114 is a selective positive allosteric modulator of M5 muscarinic acetylcholine receptor (mAChR) (EC50 = 2.7 μM for human M5, and >30 μM for M1, M2, M3 and M4, receptors). Synonyms: VU 0365114; VU0365114; VU-0365114; 1-[(1,1'-Biphenyl)-4-ylmethyl]-5-(trifluoromethoxy)-1H-indole-2,3-dione; 1-[(4-phenylphenyl)methyl]-5-(trifluoromethoxy)indole-2,3-dione. Grades: ≥98% by HPLC. CAS No. 1208222-39-2. Molecular formula: C22H14F3NO3. Mole weight: 397.35.
VU 0409106
VU 0409106 is a potent and selective mGlu5 negative allosteric modulator (IC50 = 49 nM for human mGlu5) with selectivity over a panel of GPCRs and ion channels. VU 0409106 exhibits no significant nonspecific binding in rat brain homogenates in vitro. Synonyms: VU0409106, VU 0409106, VU-0409106; 3-Fluoro-N-(4-methyl-2-thiazolyl)-5-(5-pyrimidinyloxy)benzamide. Grades: ≥98% by HPLC. CAS No. 1276617-62-9. Molecular formula: C15H11FN4O2S. Mole weight: 330.34.
VU 0422288
VU 0422288 is a group III mGlu receptor positive allosteric modulator (EC50 = 108, 125 and 146 nM for mGlu4, mGlu8 and mGlu7, respectively) with selectivity over a panel of 68 other GPCRs, ion channels and transporters. VU 0422288 has been shown to potentiate mGlu7-mediated reductions in excitatory post synaptic potentials in hippocampal slices. Synonyms: VU0422288; VU-0422288; VU 0422288; ML 396; ML-396; ML396; N-[3-Chloro-4-[(5-chloro-2-pyridinyl)oxy]phenyl]-2-pyridinecarboxamide. Grades: ≥98% by HPLC. CAS No. 1630936-95-6. Molecular formula: C17H11Cl2N3O2. Mole weight: 360.19.
VU0453379
VU0453379 is a highly selective and central nervous system (CNS) permeability positive allosteric modulator (PAM) of glucagon-like peptide-1R (GLP-1R) with an EC50 of 1.3 μM. Synonyms: VU-0453379; VU 0453379. Grades: ≥98% by HPLC. CAS No. 1638646-27-1. Molecular formula: C26H34N4O2. Mole weight: 434.6.
VU 0469650 hydrochloride
VU 0469650 hydrochloride is a potent and selective negative allosteric modulator of mGlu1 (IC50 = 99 nM), displaying >100-fold selectivity for mGlu1 over mGlu2-8 and 68 other GPCRs, ion channels, kinases and transporters. Synonyms: VU 0469650 hydrochloride, VU 0469650 HCl, VU 0469650, VU0469650, VU-0469650; 3-[(3R)-3-Methyl-4-(tricyclo[3.3.1.13,7]dec-1-ylcarbonyl)-1-piperazinyl]-2-pyridinecarbonitrile hydrochloride. Grades: ≥98% by HPLC. CAS No. 1443748-47-7. Molecular formula: C22H28N4O.HCl. Mole weight: 400.94.
VU 0650991
VU 0650991 is a selective and non-competitive glucagon-like peptide-1 (GLP-1) receptor antagonist with IC50 value of 650 nM. Synonyms: GLP-1R Antagonist 1; 7-(4-Chlorophenyl)-5,8-dihydro-1,3-dimethyl-5,5-bis(trifluoromethyl)pyrimido[4,5-d]pyrimidine-2,4(1H,3H)-dione. Grades: ≥98% by HPLC. CAS No. 488097-06-9. Molecular formula: C16H11ClF6N4O2. Mole weight: 440.73.
VU 10010
VU 10010 is a selective allosteric potentiator at M4 acetylcholine receptors (EC50 = 33 and 0.7 nM for ACh in the absence and presence of VU10010 respectively). VU 10010 binds to an allosteric site on the receptor increasing affinity for ACh and coupling to G-proteins. Synonyms: VU 10010; VU10010; VU-10010; 3-Amino-N-[(4-chlorophenyl)methyl]-4,6-dimethylthieno[2,3-b]pyridine-2-carboxamide. Grades: ≥99% by HPLC. CAS No. 633283-39-3. Molecular formula: C17H16ClN3OS. Mole weight: 345.85.
VU 1545
VU 1545 is a metabotropic glutamate receptor 5 (mGlu5) positive allosteric modulator (EC50 = 9.6 nM, Ki = 156 nM at rat mGlu5). Synonyms: VU-1545, VU 1545, VU1545; N-[1-(2-Fluorophenyl)-3-phenyl-1H-pyrazol-5-yl]-4-nitrobenzamide. Grades: ≥98% by HPLC. CAS No. 890764-63-3. Molecular formula: C22H15FN4O3. Mole weight: 402.38.
VU 29
VU 29 is a potent positive allosteric potentiator at the rat mGlu5 receptor (EC50 = 9 nM) with selectivity for mGlu5 over mGlu1 and mGlu2 receptors (EC50 = 557 nM and 1.51 μM for mGlu1 and mGlu2, respectively). VU 29 binds to the MPEP allosteric site (Ki app = 244 nM). VU 29 was shown to potentiate both DHPG-induced LTP and threshold θ-burst stimulation (TBS)-induced LTP in rat hippocampal slices. Synonyms: N-(1,3-Diphenyl-1H-pyrazolo-5-yl)-4-nitrobenzamide; DPAP; VU-29; VU 29; VU29; 4-nitro-N-(1,3-diphenyl-1H-pyrazol-5-yl)benzamide. Grades: ≥99% by HPLC. CAS No. 890764-36-0. Molecular formula: C22H16N4O3. Mole weight: 384.39.
VU 590 dihydrochloride
VU 590 dihydrochloride is a selective renal outer medullary potassium channel (Kir1.1, ROMK) inhibitor (IC50 = 294 nM). VU 590 displays no effect upon Kir2.1 or Kir4.1. It also inhibits the inward retifying K+ channel Kir7.1. Synonyms: VU590 HCl; VU590 dihydrochloride; VU590; VU-590; VU 590; CID-4536383; CID 4536383; CID4536383; ML 111; ML111 ; ML-111; 7,13-Bis[(4-nitrophenyl)methyl]-1,4,10-trioxa-7,13-diazacyclopentadecane dihydrochloride. Grades: ≥97% by HPLC. CAS No. 1783987-83-6. Molecular formula: C24H32N4O7.2HCl. Mole weight: 561.46.
VU 591 hydrochloride
VU 591 hydrochloride is a selective renal outer medullary potassium channel (Kir1.1, ROMK) antagonist (IC50 = 300 nM). VU 591 exhibits no effect on Kir7.1 at concentrations up to 10 μM and no inhibition of Kir2.1, Kir2.3 or Kir4.1. Synonyms: VU 591 hydrochloride; VU591 hydrochloride; VU-591 hydrochloride; 6-Nitro-2-[(6-nitro-1H-benzimidazol-2-yl)methoxymethyl]-1H-benzimidazole hydrochloride. Grades: ≥99% by HPLC. CAS No. 1315380-70-1. Molecular formula: C16H12N6O5.HCl. Mole weight: 404.76.
VU 6008667
VU 6008667 is a selective negative allosteric modulator (NAM) of M5 muscarinic acetylcholine receptor (mAChR) (IC50 values of 1.2 and 1.6 μM in human and rat M5, respectively). Moreover, VU6008667 has high CNS penetration and exhibits a desired short half-life in rats (t1/2 = 2.3 h) for addiction studies. Synonyms: VU 6008667; VU6008667; VU-6008667. Grades: 99%. CAS No. 2092923-21-0. Molecular formula: C24H17ClF2N2O2. Mole weight: 438.85.
VUF 10166
VUF 10166 is a potent and competitive 5-HT3 receptor antagonist (IC50 = 0.04 and 22 nM for human 5HT3A and 5-HT3AB receptors, respectively). VUF 10166 exhibits partial agonist activity at 5-HT3A receptors at higher concentrations (EC50 = 5.2 μM). It also acts as a histamine H4 receptor antagonist (pKi = 6.64 in HEK cells). Synonyms: VUF 10166; VUF10166; VUF-10166; 2-Chloro-3-(4-methyl-1-piperazinyl)quinoxaline. Grades: ≥98% by HPLC. CAS No. 155584-74-0. Molecular formula: C13H15ClN4. Mole weight: 262.74.
VUF10460
VUF10460 is a specific non-imidazole histamine H4 receptor agonist (pKi = 7.46, 8.22 for rat H4 receptor and human H4 receptor respectively) with 50-fold selectivity over the H3 subtype (pKi = 5.75). Synonyms: VUF10460; VUF 10460; VUF-10460; 4-(4-methylpiperazin-1-yl)-6-phenylpyrimidin-2-amine. CAS No. 1028327-66-3. Molecular formula: C15H19N5. Mole weight: 269.34.
VUF 11207 fumarate
VUF 11207 fumarate is a potent ACKR3 (CXCR7) agonist. Synonyms: VUF 11207 fumarate; VUF11207 fumarate; VUF-11207 fumarate; N-[(2E)-3-(2-Fluorophenyl)-2-methyl-2-propen-1-yl]-3,4,5-trimethoxy-N-[2-(1-methyl-2-pyrrolidinyl)ethyl]benzamide fumarate. CAS No. 1785665-61-3. Molecular formula: C27H35FN2O4.C4H4O4. Mole weight: 586.65.
VUF 11207 trifluoroacetate salt
VUF 11207 is a potent agonist of the G protein-coupled chemokine receptor 7 (CXCR7). It also reduces CXCR7 cell surface expression (EC50 = 14.1 nM) in vitro. Synonyms: VUF11207 TFA salt. Grades: ≥95%. Molecular formula: C27H35FN2O4·CF3COOH. Mole weight: 584.6.
VUF 11222
VUF 11222 is a high affinity non-peptide CXCR3 agonist (pKi = 7.2). Synonyms: VUF-11222, VUF 11222, VUF11222; 2'-Bromo-N-[[(1R,5S)-6,6-dimethylbicyclo[3.1.1]hept-2-en-2-yl]methyl]-N,N-dimethyl-[1,1'-biphenyl]-4-methanaminium iodide. CAS No. 1414376-84-3. Molecular formula: C25H31BrIN. Mole weight: 552.33.
VUF 5574
VUF 5574 is a potent and competitive antagonist for the human adenosine A3 receptor (Ki = 4 nM) that displays ≥ 2500-fold selectivity over A1 and A2A receptors. Synonyms: VUF5574, VUF 5574, VUF-5574; N-(2-Methoxyphenyl)-N'-[2-(3-pyrindinyl)-4-quinazolinyl]-urea; 1-(2-Methoxyphenyl)-3-(2-(pyridin-3-yl)quinazolin-4-yl)urea. Grades: ≥98% by HPLC. CAS No. 280570-45-8. Molecular formula: C21H17N5O2. Mole weight: 371.39.
VUF 5681 dihydrobromide
VUF 5681 dihydrobromide is a potent histamine H3 receptor silent antagonist (pKi = 8.35). Synonyms: VUF 5681 dihydrobromide; VUF5681 dihydrobromide; VUF-5681 dihydrobromide; 4-[3-(1H-Imidazol-4-yl)propyl]piperidine dihydrobromide. Grades: ≥98% by HPLC. CAS No. 639089-06-8. Molecular formula: C11H19N3.2HBr. Mole weight: 355.11.
VUF 8430 dihydrobromide
VUF 8430 dihydrobromide is a high affinity (pKi = 7.5) and potent histamine H4 receptor full agonist (pEC50 = 7.3). VUF 8430 also has moderate affinity for H3 receptors (pKi = 6.0) and weak partial agonist activity at H2 receptors. Synonyms: VUF8430 dihydrobromide; VUF-8430 dihydrobromide; VUF 8430 dihydrobromide; 2-[(Aminoiminomethyl)amino]ethyl carbamimidothioic acid ester dihydrobromide; S-(2-guanidylethyl)-isothiourea; S,2-Guanidinoethylisothiuronium bromide hydrobromide. CAS No. 100130-32-3. Molecular formula: C4H11N5S.2HBr. Mole weight: 323.05.
VX-11e
VX-11e is a potent, selective, and orally bioavailable inhibitor of ERK, which is extracellular signal-regulated kinases. It is an antitumor agent and potently blocks proliferation of HT29 cells. Synonyms: VX-11e; VX 11e; VX11e; VTX-11e; VTX11e; VTX 11e; ERK-11e; ERK 11e; ERK11e. Grades: >98%. CAS No. 896720-20-0. Molecular formula: C24H20Cl2FN5O2. Mole weight: 500.35.
VX-166
VX-166 is a caspase inhibitor and can be used as a novel potential treatment for sepsis. VX-166 can also reduce fibrosis in an animal model of nonalcoholic steatohepatitis. Uses: Sepsis. Synonyms: VX166, VX 166, VX-166; (S)-3-((S)-2-(3-((methoxycarbonyl)amino)-2-oxopyridin-1(2H)-yl)butanamido)-4-oxo-5-(2,3,5,6-tetrafluorophenoxy)pentanoic acid. Grades: 98%. CAS No. 800408-39-3. Molecular formula: C22H21F4N3O8. Mole weight: 531.41.
VX-222 (VCH-222, Lomibuvir)
VX-222 (VCH-222) is a novel, potent and selective inhibitor of HCV polymerase with IC50 of 0.94-1.2 μM, 15.3-fold less effective for mutant M423T, and 108-fold less effective for mutant I482L. Phase 2. Synonyms: 2-Thiophenecarboxylic acid, 5-(3,3-dimethyl-1-butyn-1-yl)-3-[(cis-4-hydroxycyclohexyl)[(trans-4-methylcyclohexyl)carbonyl]amino]-; 5-(3,3-Dimethyl-1-butyn-1-yl)-3-[(cis-4-hydroxycyclohexyl)[(trans-4-methylcyclohexyl)carbonyl]amino]-2-thiophenecarboxylic acid; Lomibuvir; VCH 222; VX 222; VX222. Grades: >98%. CAS No. 1026785-59-0. Molecular formula: C25H35NO4S. Mole weight: 445.61.
VX-702
VX-702 is a highly selective inhibitor of p38α MAPK, 14-fold higher potency against the p38α versus p38&beta. Synonyms: VX-702; VX 702; VX702. Grades: >98%. CAS No. 745833-23-2. Molecular formula: C19H12F4N4O2. Mole weight: 404.3.
VX-745
VX 745 is a potent and selective inhibitor of p38α mitogen-activated protein (MAP) kinase. VX 745 is a potential anti-inflammatory agents. Studies suggest that VX 745 may be useful in the treatment of Werner syndrome. Synonyms: VX-745; VX 745; VX745; VRT-031745, VD-31745; VRT 031745, VD 31745; VRT031745, VD31745; Neflamapimod. Grades: 0.97. CAS No. 209410-46-8. Molecular formula: C19H9Cl2F2N3OS. Mole weight: 436.258.
VX-787
VX-787, a pyrrolopyridine derivative, has been found to be an antiviral agent and is still under Phase II trial against Influenza A virus infection. Synonyms: VX-787; VX 787; VX787; JNJ-872; JNJ 872; JNJ872; VRT-0928787; VRT 0928787; VRT0928787;pimodivir; (2S,3S)-3-((5-Fluoro-2-(5-fluoro-1H-pyrrolo[2,3-b]pyridin-3-yl)pyrimidin-4-yl)amino)bicyclo[2.2.2]octane-2-carboxylic Acid. Grades: 98%. CAS No. 1629869-44-8. Molecular formula: C20H19F2N5O2. Mole weight: 399.40.
W-84 dibromide
W-84 dibromide is a potent allosteric modulator of muscarinic M2 receptors. W-84 dibromide has been shown to stabilize cholinergic antagonist-receptor complexes by an allosteric effect, and enhance the protective effect of atropine against organophosphate poisoning. Synonyms: W-84 dibromide; W 84 dibromide; W84 dibromide; Hexamethylene-bis-[dimethyl-(3-phthalimidopropyl)ammonium]dibromide. CAS No. 21093-51-6. Molecular formula: C32H44Br2N4O4. Mole weight: 708.53.
Walrycin B
Walrycin B is a novel antibacterial compound specifically targeting the essential WalR response regulator. It is known as an analog of toxoflavin, which has been shown to have a strong MIC for B. subtilis and S. aureus but whose mode of action is not clear. It could also interact with WalR to cause bactericidal effects. Synonyms: Walrycin B; 878419-78-4; Walrycin-B; 1,6-dimethyl-3-(4-(trifluoromethyl)phenyl)pyrimido[5,4-e][1,2,4]triazine-5,7(1H,6H)-dione; CHEMBL1096283; 1,6-dimethyl-3-[4-(trifluoromethyl)phenyl]pyrimido[5,4-e][1,2,4]triazine-5,7-dione; 4-tert.Butylcalix[6]arene; SCHEMBL3472472; GTPL11256; EX-A363; XRVMPTWWKLKLPB-UHFFFAOYSA-N; BCP09097; BDBM50438912; MFCD07188899; AKOS001872828; NCGC00371145-02; AC-35969; BS-17871; HY-18219; FT-0700392; S0195; A862391; EN300-18666475; SR-01000100642; J-690379; SR-01000100642-1; D052-0142; 1,6-dimethyl-3-[4-(trifluoromethyl)phenyl]-1H,5H,6H,7H-pyrimido[5,4-e][1,2,4]triazine-5,7-dione. Grades: >98%. CAS No. 878419-78-4. Molecular formula: C14H10F3N5O2. Mole weight: 337.26.
Watanipidine monohydrochloride
Watanipidine, also called as AE 0047 or Calbren, is a calcium channel antagonist. Synonyms: 5-O-[2-[4-(4-benzhydrylpiperazin-1-yl)phenyl]ethyl] 3-O-methyl 2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate;hydrochloride; 3,5-Pyridinedicarboxylic acid, 1,4-dihydro-2,6-dimethyl-4-(3-nitrophenyl)-, 2-(4-(4-(diphenylmethyl)-1-piperazinyl)phenyl)ethyl methyl ester, monohydrochloride; Watanipidine HCl. CAS No. 116308-56-6. Molecular formula: C41H43ClN4O6. Mole weight: 723.26.
Way 100135
Way 100135 is a selective 5-HT1A receptor antagonist originated by Wyeth with IC50 value of 15 nM. IC 50 values for 5-HT1B, 1C, 2,α1, α2 and D2 receptors are over 1000 nM. No preclinical development for Anxiety disorders in USA was reported. Uses: Anxiety disorders. Synonyms: Way100135; Way-100135; Way 100135; N-(tert-butyl)-3-(4-(2-methoxyphenyl)piperazin-1-yl)-2-phenylpropanamide;(S)-WAY 100135 dihydrochloride(149007-54-5). Grades: 98%. CAS No. 133025-23-7. Molecular formula: C24H33N3O2. Mole weight: 395.54.
(-)-WAY 100135 dihydrochloride
(-)-WAY 100135 dihydrochloride is a selective serotonin 5-HT1A antagonist. Synonyms: WAY 100135 dihydrochloride; WAY100135 dihydrochloride; WAY-100135 dihydrochloride; (2R)-N-tert-butyl-3-[4-(2-methoxyphenyl)piperazin-1-yl]-2-phenylpropanamide dihydrochloride. Grades: 99%. CAS No. 149007-53-4. Molecular formula: C24H33N3O2.2HCl. Mole weight: 468.46.
WAY 100135 dihydrochloride
WAY 100135 dihydrochloride is a selective 5-HT1A antagonist (IC50 = 15 nM). Uses: Serotonin antagonists. Synonyms: WAY 100135 hydrochloride; WAY100135 hydrochloride; WAY-100135 hydrochloride; 3-[4-(2-Methoxyphenyl)piperazin-1-yl]-2-phenyl-N-tert-butyl-propanamide dihydrochloride; N-tert-Butyl-3-(4-(2-methoxyphenyl)-piperazin-1-yl)-2-phenylpropanamide dihydrochloride. Grades: 99%. CAS No. 149055-79-8. Molecular formula: C24H33N3O2.2HCl. Mole weight: 468.46.
Way 100289
Way 100289 is a selective Serotonin 3 receptor antagonist originated by Wyeth. No development for the treatment of Anxiety disorders, Learning disorders and Psychotic disorders was reported. Uses: Anxiety disorders; learning disorders; psychotic disorders. Synonyms: Way 100289; Way-100289; Way100289; 2-(cyclopropylmethoxy)-N-((8-methyl-8-azabicyclo[3.2.1]octan-3-yl)carbamoyl)benzamide. Grades: 98%. CAS No. 136013-69-9. Molecular formula: C20H27N3O3. Mole weight: 357.45.
WAY-100635
WAY-100635 is an achiral analogue of WAY-100135 which is significantly more potent and selective than the latter compound and which displays unequivocal 5-HTIA receptor antagonist activity in a range of pre-(somatodendritic) and postsynaptic functional mo. Synonyms: WAY-100635; WAY100635; WAY 100635. N- [2- [4- (2-methoxyphenyl) piperazin-1-yl] ethyl] -N-pyridin-2-ylcyclohexane carboxamidecyclohexane carboxamide, N-(2-(4-(2-methoxyphenyl)-1-piperazinyl)ethyl)-N-2-pyridinyl-N-(2-(4-(2-methoxyphenyl)-1-piperazinyl)ethyl)-N-(2-pyridinyl)cyclohexanecarboxamide. CAS No. 162760-96-5. Molecular formula: C25H34N4O2. Mole weight: 422.56.
WAY 100635 hydrochloride
WAY 100635 hydrochloride is a 5-HT1A receptor antagonist with dopamine D4 agonist activity (Ki values 2.2 nM, 6260 nM, 24 nM, >10,000 nM, 20 nM, 322 nM, and 16 nM for 5-HT1A, 5-HT2A, 5-HT2B, 5-HT7, α1A, α1B, and D4, respectively). Uses: Serotonin antagonists. Synonyms: WAY 100635 trihydrochloride; WAY100635 trihydrochloride; WAY-100635 trihydrochloride; N-[2-[4-(2-methoxyphenyl)piperazin-1-yl]ethyl]-N-pyridin-2-ylcyclohexanecarboxamide trihydrochloride. Grades: 99%. CAS No. 146714-97-8. Molecular formula: C25H34N4O2.3HCl. Mole weight: 531.947.
Way 123398
Way 123398 is a class III antiarrhythmic agent. It is a Potassium channel antagonist originated by Wyeth. No preclinical development for Arrhythmias in USA was reported. Uses: Arrhythmias. Synonyms: Way 123398; Way123398; Way-123398; N-methyl-N-(2-(methyl(1-methyl-1H-benzimidazol-2-yl)amino)ethyl)-4-((methylsulfonyl)amino)-Benzenesulfonamide. Grades: 98%. CAS No. 138490-53-6. Molecular formula: C19H25N5O4S2. Mole weight: 451.57.
WAY-126299A
WAY-126299A, a benzothiazoly derivative, has been found to be a 5-lipoxygenase inhibitor as well as Leukotriene D4 receptor antagonist and was once studied in Asthma. Synonyms: WAY 126299A; WAY-126299A; WAY126299A; 2-Naphthaleneacetamide, 6-(2-benzothiazolylmethoxy)-N-hydroxy-N,alpha-dimethyl-, sodium salt, (S)-; 2-Naphthaleneacetamide, 6-(2-benzothiazolylmethoxy)-N-hydroxy-N,alpha-dimethyl-, sodium salt, (alphaS)-. Grades: 98%. CAS No. 169626-43-1. Molecular formula: C22H19N2NaO3S. Mole weight: 414.45.
WAY-161503
WAY-161503 is a full agonist of 5-HT2C receptors that exhiits ~6-fold less potent at 5-HT2A receptors (Ki = 18 nM) and 20-fold less potent at 5-HT2B receptors (Ki = 60 nM). Synonyms: WAY 161503; WAY161503; 8,9-Dichloro-2,3,4,4A-tetrahydro-1H-pyrazino[1,2-A]quinoxalin-5(6H)-one hydrochloride. Grades: 98%. CAS No. 75704-24-4. Molecular formula: C11H11Cl2N3O. Mole weight: 272.13.
WAY 161503 hydrochloride
WAY 161503 hydrochloride is a potent and selective 5-HT2C receptor agonist (Ki = 4 nM; EC50 = 12 nM). Synonyms: WAY 161503 hydrochloride; WAY161503 hydrochloride; WAY-161503 hydrochloride; 8,9-Dichloro-2,3,4,4a-tetrahydro-1H-pyrazino[1,2-a]quinoxalin-5(6H)-one hydrochloride. Grades: ≥99% by HPLC. CAS No. 276695-22-8. Molecular formula: C11H11Cl2N3O.HCl. Mole weight: 308.59.
WAY 170523
WAY 170523 is a potent and selective inhibitor of MMP-13 (IC50 = 17, 945, > 1000 and > 10000 nM for MMP-13, MMP-9, TACE and MMP-1 respectively). Synonyms: WAY-170523; WAY 170523; WAY170523; N-[2-[4-[[[2-[ (Hydroxyamino) carbonyl]-4, 6-dimethylphenyl] (phenylmethyl) amino]sulfonyl]phenoxy]ethyl]-2-benzofurancarboxamide. Grades: ≥99% by HPLC. CAS No. 307002-73-9. Molecular formula: C33H31N3O7S. Mole weight: 613.68.
WAY181187
WAY181187 is a potent and selective 5-HT6 receptor full agonist. It possesses high affinity binding at the human 5-HT6 receptor and profile as full receptor agonists. It induces robust increases in extracellular GABA levels in the frontal cortex, striatum, hippocampus and amygdala of rats. It has modest to no effects on norepinephrine, serotonin, dopamine, or glutamate levels. It has demonstrated preclinical efficacy in rodent models of depression, anxiety, and notably obsessive-compulsive disorder. Uses: Way181187 has demonstrated preclinical efficacy in rodent models of depression, anxiety, and notably obsessive-compulsive disorder. Synonyms: WAY-181187; WAY 181187; WAY181187;2-(1-((6-Chloroimidazo(2,1-b)(1,3)thiazol-5-yl)sulfonyl)-1H-indol-3-yl)ethylamine;SAX-187;SAX187; SAX 187. Grades: 98%. CAS No. 554403-49-5. Molecular formula: C15H13ClN4O2S2. Mole weight: 380.86.
WAY 181187 oxalate
WAY 181187 oxalate is a selective and high affinity 5-HT6 agonist with 60-fold selectivity over other 5-HT and monoamine receptors. Synonyms: WAY 181187 oxalate; WAY181187 oxalate; WAY-181187 oxalate; 1-[(6-Chloroimidazo[2,1-b]thiazol-5-yl)sulfonyl]-1H-indole-3-ethanamine oxalate. Grades: ≥98% by HPLC. CAS No. 1883548-85-3. Molecular formula: C15H13ClN4O2S2.C2H2O4. Mole weight: 470.91.
WAY-200070
WAY-200070 is a selective estrogen receptor β (ERRβ) agonist (IC50 = 2.3 nM) that exhibit 68-fold selectivity over ERα (EC50 = 155 nM for ERα). Synonyms: 4-(7-bromo-5-hydroxy-3H-1,3-benzoxazol-2-ylidene)cyclohexa-2,5-dien-1-one; Br-ERb-041; WAY 200070; WAY 20070-3; WAY-200070; WAY-200070-3; WAY200070; WAY200070-3. CAS No. 440122-66-7. Molecular formula: C13H8BrNO3. Mole weight: 306.11.
WAY 208466 dihydrochloride
WAY 208466 dihydrochloride is a high affinity and selective 5-HT6 agonist (EC50 = 7.3 nM at the human 5-HT6 receptor) with antidepressant and anxiolytic activity. WAY 208466 dihydrochloride was shown to increase cortical GABA levels in vivo in rat frontal cortex. Synonyms: WAY-208466 2HCl; WAY 208466 2HCl; WAY208466 2HCl; WAY-208466 dihydrochloride; WAY 208466 dihydrochloride; WAY208466 dihydrochloride; 3-[(-3-Fluorophenyl)sulfonyl]-N,N-dimethyl-1H-pyrrolo[2,3-b]pyridine-1-ethanamine dihydrochloride. Grades: ≥99% by HPLC. CAS No. 1207064-61-6. Molecular formula: C17H18FN3O2S.2HCl. Mole weight: 420.33.
WAY-262611
WAY-262611 is a wingless beta-Catenin agonist that increases bone formation rate. Synonyms: WAY262611 2HCl; WAY262611 2HCl; WAY-262611 2HCl; WAY 262611 dihydrochloride; WAY-262611 dihydrochloride WAY 262611 dihydrochloride. Grades: >98%. CAS No. 1123231-07-1. Molecular formula: C20H22N4. Mole weight: 318.42.
WAY 262611 dihydrochloride
WAY 262611 dihydrochloride is an inhibitor of Dickkopf-1 (DKK1), which antagonizes Wnt/β-Catenin signaling. DKK1 is a soluble inhibitor of Wnt-3a mediated Wnt/β-catenin signaling required for embryonic head development. Inhibition of DKK1 by WAY 262611 activates the Wnt signaling pathway and stimulates β-catenin/TCF-dependent transcription with an EC50 value of 0.63 μM. Synonyms: WAY-262611 dihydrochloride; WAY 262611 dihydrochloride; WAY262611 dihydrochloride; (1-(4-(naphthalen-2-yl)pyrimidin-2-yl)piperidin-4-yl)methanamine dihydrochloride. Grades: 99%. Molecular formula: C20H22N4.2HCl. Mole weight: 391.34.
WAY-600
WAY-600 is a potent, ATP-competitive and selective inhibitor of mTOR with IC50 of 9 nM. Synonyms: WAY 600; WAY600. Grades: 98%. CAS No. 1062159-35-6. Molecular formula: C28H30N8O. Mole weight: 494.603.
WAY 629 hydrochloride
WAY 629 hydrochloride is a selective 5-HT2C agonist (Ki = 56, 2350, 1575 and 815 nM for human recombinant 5-HT2C, 5-HT2A, 5-HT6 and 5-HT7 receptors, respectively). WAY 629 promotes intracellular Ca2+ mobilization in CHO cells expressing human 5-HT2C receptors (EC50 = 72 nM). Synonyms: [1,4]Diazepino[6,7,1-jk]carbazole, 4,5,6,7,9,10,11,12-octahydro-, hydrochloride (1:1); WAY629 hydrochloride; WAY-629 hydrochloride; 1,2,3,4,8,9,10,11-Octahydro[1,4]diazepino[6,7,1-jk]carbazole hydrochloride; [1,4]Diazepino[6,7,1-jk]carbazole, 1,2,3,4,8,9,10,11-octahydro-, monohydrochloride. Grades: ≥98% by HPLC. CAS No. 57756-44-2. Molecular formula: C15H18N2.HCl. Mole weight: 262.78.
WB 4101 hydrochloride
WB 4101 hydrochloride is a selective α1A-adrenergic receptor antagonist. Synonyms: WB 4101; WB-4101; WB4101; WB 4101 hydrochloride; WB 4101 HCl. 2-(2,6-Dimethoxyphenoxyethyl)aminomethyl-1,4-benzodioxane hydrochloride. Grades: ≥99% by HPLC. CAS No. 2170-58-3. Molecular formula: C19H23NO5.HCl. Mole weight: 381.86.
WDR5-0103
WDR5-0103 is a small molecule that binds a peptide-binding pocket on WDR5 with Kd of 450 nM. It inhibits MLL catalytic activity with an IC50 value of 39±10 μM in vitro. It is a WD40-repeat antagonist that binds to WDR55 central cavity. It inhibits MLL1 histone methyltransferase activity in vitro through disruption of the interaction of MLL with WDR5. It is an essential componet of the human trithorax-like famliy of SET1 methyltransferase complexes that carry out trimethylation of histone 3 Lys4. Uses: Wdr5-0103 inhibits mll1 histone methyltransferase activity. it is an essential componet of the human trithorax-like famliy of set1 methyltransferase complexes that carry out trimethylation of histone 3 lys4. Synonyms: 3-[(3-Methoxybenzoyl)aMino]-4-(4-Methyl-1-piperazinyl)benzoic Acid Methyl Ester;Methyl 3-(3-methoxybenzamido)-4-(4-methylpiperazin-1-yl)benzoate;WDR5-0103; WDR 5-0103; WDR-5-0103; WDR50103; WDR-50103; WDR 50103; WD-Repeat Protein 5-0103. Grades: >98 %. CAS No. 890190-22-4. Molecular formula: C21H25N3O4. Mole weight: 383.44.
WEB 2086
WEB 2086 is a potent and selective platelet-activating factor (PAF) receptor antagonist (Ki = 16.3 nM) potentially used for the treatment of asthma and allergic rhinitis (AR). WEB 2086 exhibits an inhibitory effect on growth and proliferation of MCF-7 breast cancer cells. Uses: Platelet aggregation inhibitors. Synonyms: DE-081; DE 081; DE081; WEB-2086; WEB2086; WEB2086; WEB-2086BS; Apafant. Apafant; 4-[3-[4[(2-Chlorophenyl)-9-methyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a]diazepin-2-yl]-1-oxopropyl]morpholine. Grades: ≥99% by HPLC. CAS No. 105219-56-5. Molecular formula: C22H22N5O2SCl. Mole weight: 455.96.
WEHI-345 analogue
An analogue of WEHI-345, a pyrazolo-pyridine derivative, is a protein kinase inhibitor and could be significant for studying the mechanism of cancer. Uses: An analogue of wehi-345 is a protein kinase inhibitor and could be significant for studying the mechanism of cancer. Synonyms: WEHI-345 (analog); SCHEMBL727021; CS-5569; WEHI 345 (analog); SCHEMBL 727021; CS 5569; WEHI345 (analog); SCHEMBL 727021; CS5569. Grades: 98%. CAS No. 1354825-62-9. Molecular formula: C23H25N7O. Mole weight: 415.49.
WEHI-539
WEHI-539, a selective BCL-XL inhibitor that can be function as a single-agent inducer of apoptosis while sparing normal cells, it leads to MOMP and apoptosis due to displacing bound activator BH3s or monomeric BAX and BAK from BCL-XL to induce the homo-ol. Synonyms: 4-Thiazolecarboxylic acid, 5-[3-[4-(aminomethyl)phenoxy]propyl]-2-[8-[2-(2-benzothiazolyl)hydrazinylidene]-5,6,7,8-tetrahydro-2-naphthalenyl]-; 5-[3-[4-(Aminomethyl)phenoxy]propyl]-2-[8-[2-(2-benzothiazolyl)hydrazinylidene]-5,6,7,8-tetrahydro-2-naphthalenyl]-4-thiazolecarboxylic acid; WEHI 539; WEHI539; 5-(3-(4-(aminomethyl)phenoxy)propyl)-2-(8-(2-(benzo[d]thiazol-2-yl)hydrazineylidene)-5,6,7,8-tetrahydronaphthalen-2-yl)thiazole-4-carboxylic acid. Grades: ≥95%. CAS No. 1431866-33-9. Molecular formula: C31H29N5O3S2. Mole weight: 583.73.
WEHI-539 hydrochloride
WEHI-539 is a selective BCL-XL inhibitor that can function as a single-agent inducer of apoptosis while sparing normal cells. WEHI-539 provokes BAK-mediated apoptosis in BCL-XL-dependent cells. Synonyms: 4-Thiazolecarboxylic acid, 5-[3-[4-(aminomethyl)phenoxy]propyl]-2-[8-[2-(2-benzothiazolyl)hydrazinylidene]-5,6,7,8-tetrahydro-2-naphthalenyl]-, hydrochloride (1:1); 5-(3-(4-(aminomethyl)phenoxy)propyl)-2-(8-(2-(benzo[d]thiazol-2-yl)hydrazineylidene)-5,6,7,8-tetrahydronaphthalen-2-yl)thiazole-4-carboxylic acid hydrochloride; WEHI-539 HCl; 5-{3-[4-(Aminomethyl)phenoxy]propyl}-2-[8-(1,3-benzothiazol-2-ylhydrazono)-5,6,7,8-tetrahydro-2-naphthalenyl]-1,3-thiazole-4-carboxylic acid hydrochloride (1:1); WEHI539 hydrochloride; WEHI 539 hydrochloride. Grades: ≥95%. CAS No. 2070018-33-4. Molecular formula: C31H29N5O3S2.HCl. Mole weight: 620.18.