| Identification | Back Directory | [Name]
BMS-929075 | [CAS]
1217338-97-0 | [Synonyms]
BMS-929075
BMS-929075, 10 mM in DMSO
4-Fluoro-2-(4-fluorophenyl)-n-methyl-5-(2-methyl-5-((1-(pyrimidin-2-yl)cyclopropyl)carbamoyl)phenyl)benzofuran-3-carboxamide
3-Benzofurancarboxamide, 4-fluoro-2-(4-fluorophenyl)-N-methyl-5-[2-methyl-5-[[[1-(2-pyrimidinyl)cyclopropyl]amino]carbonyl]phenyl]- | [Molecular Formula]
C31H24F2N4O3 | [MDL Number]
MFCD31556637 | [MOL File]
1217338-97-0.mol | [Molecular Weight]
538.54 |
| Hazard Information | Back Directory | [Uses]
BMS-929075 is a potent and orally active HCV NS5B replicase palm site allosteric inhibitor. BMS-929075 shows high oral bioavailability. BMS-929075 shows cytotoxicity[1]. | [in vivo]
BMS-929075 (compound 37) (2 mg/kg for i.v.; 6 mg/kg for p.o.) shows good pharmacokinetic parameters with oral bioavailability of 48% in rats[1].
Pharmacokinetic Parameters of BMS-929075 in Male Sprague-Dawley rats[1].
| IV | | | PO | | | | | | | | species | Cl (mL/min/kg) | IV t1/2(hr) | Vss(L/kg) | Cmax(μM) | Tmax(hr) | AUC (μM h) | C6 liver (μM) | C24 liver (μM) | C24 liver/plasma (μM) | F% (mL/min/kg) | | rat | 1.7 | 4.7 | 0.7 | 7.5 | 4 | 54.5 | 15.1 | 1.12 | 1.6 | 48 |
Rats, 2 mg/kg i.v.; 6 mg/kg p.o. [1].
| [References]
[1] Yeung KS, et al. Discovery of a Hepatitis C Virus NS5B Replicase Palm Site Allosteric Inhibitor (BMS-929075) Advanced to Phase 1 Clinical Studies. J Med Chem. 2017 May 25;60(10):4369-4385. DOI:10.1021/acs.jmedchem.7b00328 |
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