Narlaprevir

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种有效的第二代 HCV NS3 丝氨酸蛋白酶抑制剂，Ki 为 6 nM。

A potent, second generation HCV NS3 serine protease inhibitor with Ki of 6 nM; displays no significant issues in the in vitro CYP or hERG assay; shows replicon EC90 of 40 nM; exhibits improved potency (～10-fold over Boceprevir), pharmacokinetic profile and physicochemical characteristics.

Narlaprevir (SCH 900518) potently inhibits ketoamide with a Ki value of 7 nM.Narlaprevir (SCH 900518) potently inhibits replicon RNA with an EC90 value of 40 nM.

Pharmacokinetic Analysis Narlaprevir (SCH 900518) exhibits middle oral bioavailability (rat 46%, dog 29%, monkey 46 %) following oral administration (rat 10 mg/kg, dog 3 mg/kg, monkey 3 mg/kg ).Narlaprevir (SCH 900518) exhibits moderate half-lives (rat 4.8 and dog 2 h) following intravenous administration (rat 4 and dog 1 mg/kg). Animal Model:rats, dogs, monkeys Dosage:Rat PO/IV 10/4 mg/kg; dog PO/IV 3/1 mg/kg; monkey PO 3 mg/kgAdministration:Intravenous (i.v.) or oral gavage Result:T1/2s of 4.8 and 2 h for rats and dogs, respectively.

SCH 900518 | SCH900518 | SCH-900518

Microbiology/Virology

HCV

HCV

Infection

——

865466-24-6

707.9639

C36H61N5O7S

>98% (HPLC)

10 mM in DMSO

O=C([C@@H]1[C@@]2([H])C(C)(C)[C@@]2([H])CN1C([C@H](C(C)(C)C)NC(NC3(CS(=O)(C(C)(C)C)=O)CCCCC3)=O)=O)N[C@H](C(C(NC4CC4)=O)=O)CCCC

3-Azabicyclo[3.1.0]hexane-2-carboxamide, N-[(1S)-1-[2-(cyclopropylamino)-2-oxoacetyl]pentyl]-3-[(2S)-2-[[[[1-[[(1,1-dimethylethyl)sulfonyl]methyl]cyclohexyl]amino]carbonyl]amino]-3,3-dimethyl-1-oxobutyl]-6,6-dimethyl-, (1R,2S,5S)-

(-20℃)

With Ice Pack

≥ 2 years