Elbasvir  (Synonyms: MK-8742)

Elbasvir (MK-8742) is a hepatitis C virus nonstructural protein 5A (HCV NS5A) inhibitor with EC₅₀s of 4, 3 and 3 nM against genotype 1a, 1b, and 2a, respectively.

EC50: 4 nM (HCV 1a), 3 nM (HCV 1b), 3 nM (HCV 2a)^[1]

Elbasvir shows potent activity against genotype 1a and 1b replicons, with EC₉₀ of 0.006 nM for both the wild-type 1a_H77 and 1b_con1 replicons. Elbasvir inhibits genotype 3 replicons with EC₉₀ of 0.12 nM. Elbasvir (0.06 nM, 0.6 nM, and 6 nM) demonstrates dose-dependent suppression of resistant genotype 1a replicons, illustrated by the reductions in colony counts at higher doses^[1]. Elbasvir is highly potent against HCV replicons bearing NS5A sequences from GT1a, -1b, -2a(31L), -3a, -4a, -5a, and -6, with EC₅₀s in the low-picomolar range^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

882.02

Solid

C₄₉H₅₅N₉O₇

1370468-36-2

O=C([C@H](C(C)C)NC(OC)=O)N(CCC1)[C@@H]1C(N2)=NC=C2C(C=C3)=CC4=C3C5=CC6=CC(C7=CN=C([C@H]8N(C([C@H](C(C)C)NC(OC)=O)=O)CCC8)N7)=CC=C6N5[C@H](C9=CC=CC=C9)O4

Room temperature in continental US; may vary elsewhere.

• [1]. Liu R, et al. Susceptibilities of genotype 1a, 1b, and 3 hepatitis C virus variants to the NS5A inhibitor Elbasvir. Antimicrob Agents Chemother. 2015 Nov;59(11):6922-6929.  [Content Brief]

  [2]. Lahser FC, et al. The Combination of Grazoprevir, a Hepatitis C Virus (HCV) NS3/4A Protease Inhibitor, and Elbasvir, an HCV NS5A Inhibitor, Demonstrates a High Genetic Barrier to Resistance in HCV Genotype 1a Replicons. Antimicrob Agents Chemother. 2016 A  [Content Brief]