Daclatasvir

Daclatasvir (BMS-790052) is a potent and orally active HCV NS5A protein inhibitor with EC₅₀s range of 9-146 pM for multiple HCV replicon genotypes. Daclatasvir is also a organic anion transporting polypeptide 1B (OATP1B) and OATP1B3 inhibitor with IC₅₀s of 1.5 µM and 3.27 µM, respectively^[1][2][3]. IC50 & Target: EC50: 50 pM (HCV replicon genotype 1a), 9 pM (HCV replicon genotype 1b), 71 pM (HCV replicon genotype 2a), 146 pM (HCV replicon genotype 3a), 12 pM (HCV replicon genotype 4a) and 33 pM (HCV replicon genotype 5a)^[1]
Kd: 8 nM (NS5A33-202) and 210 nM (NS5A26-202)^[2]
IC50: 1.5 µM (OATP1B) and 3.27 µM (OATP1B3)^[3] In Vitro: Daclatasvir (BMS-790052) demonstrates potent inhibitory activity towards all genotypes tested, with EC₅₀ values ranging from 9 pM to 146 pM. Daclatasvir inhibits HCV replicon genotype 1a, 1b, 2a, 3a, 4a and 5a with EC₅₀ values of 50 pM, 9 pM, 71 pM, 146 pM, 12 pM and 33 pM, respectively. Daclatasvir is a potent inhibitor of the JFH-1 genotype 2a infectious virus that replicates in cell culture (EC₅₀=28 pM)^[1]. Daclatasvir (BMS-790052) binds tightly to NS5A33-202 and NS5A26-202 with K_ds of 8 nM and 210 nM, respectively^[2]. In Vivo: Daclatasvir (BMS-790052; 30 mg/kg; oral administration; daily; for 27 days) treatment reduces serum HCV RNA titers very rapidly by ~1.5 log₁₀ at day 3^[4].