ns5a-in-1

NS5A-IN-1 is a proagent of the HCV NS5A inhibitor, Pibrentasvir (ABT-530).

Velpatasvir (GS-5816), also known as GS-5816, is a potent and selective Hepatitis C virus NS5A inhibitor. GS-5816 has demonstrated pan-genotypic activity and a high barrier to resistance in HCV replicon assays. GS-5816 demonstrated pangenotypic antiviral activity in patients with genotype 1-4 HCV infection. It will be further evaluated in combination with other pangenotypic direct-acting antivirals to achieve the goal of developing a well-tolerated, highly effective treatment for all HCV genotypes.

Beclabuvir is an allosteric inhibitor that binds to thumb site 1 of the HCV NS5B RNA-dependent RNA polymerase, inhibiting recombinant NS5B proteins from HCV genotypes 1, 3, 4, and 5 (IC50 < 28 nM).

Daclatasvir (EBP 883) (BMS-790052) is a highly selective inhibitor of HCV NS5A with EC50 of 9-50 pM, for a broad range of HCV replicon genotypes and the JFH-1 genotype 2a infectious virus in cell culture. Phase 3.

NS5A-IN-3 (Compound 15) is a potent NS5A inhibitor with high efficacy against HCV genotype 1b, enhanced activity towards genotype 3a (GT 3a), and substantial metabolic stability. It exhibits superior resistance barrier compared to daclatasvir in genotype 1b [1].

NS5A-IN-2 (Compound 33) is a potent NS5A inhibitor with remarkable efficacy against HCV genotype 1b, increased activity against genotype 3a (GT 3a), and significant metabolic stability [1].

Daclatasvir Impurity C is an impurity found in Daclatasvir, a robust inhibitor of the HCV NS5A protein [1].

NS5A-IN-4 (Compound 1.12) is a pan-genotypic, orally active inhibitor of the hepatitis C virus (HCV) NS5A, with IC50 values of 1.2, 2296, 4.6, 362, 10.3, and 693 pM against genotypes gT1b, gT1a, gT2a, gT3a, gT4a, and gT5a, respectively [1].

Yimitasvir diphosphate, also known as Emitasvir, is an orally-administered inhibitor of the hepatitis C virus (HCV) nonstructural protein 5A (NS5A). It is utilized in the study of chronic hepatitis C virus infections [1].

HCV-IN-4, a potent and orally active inhibitor of HCV NS5A, demonstrates significant efficacy against genotypes GT1a, GT2b, GT3a, and the GT1a mutations Y93H and L31V. Its half-maximal effective concentrations (EC90s) are 3 pM, 0.3 nM, 0.01 nM, 0.5 nM, and 0.02 nM, respectively[1].