| Bioactivity | 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]. | ||||||||||||
| 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)Kd: 8 nM (NS5A33-202) and 210 nM (NS5A26-202)IC50: 1.5 µM (OATP1B) and 3.27 µM (OATP1B3) | ||||||||||||
| Invitro | 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 Kds 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]. Animal Model: | ||||||||||||
| Name | Daclatasvir | ||||||||||||
| CAS | 1009119-64-5 | ||||||||||||
| Formula | C40H50N8O6 | ||||||||||||
| Molar Mass | 738.88 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Min Gao, et al. Chemical genetics strategy identifies an HCV NS5A inhibitor with a potent clinical effect. Nature. 2010 May 6;465(7294):96-100. [2]. David B Ascher, et al. Potent hepatitis C inhibitors bind directly to NS5A and reduce its affinity for RNA. Sci Rep. 2014 Apr 23;4:4765. [3]. Tomomi Furihata, et al. Different interaction profiles of direct-acting anti-hepatitis C virus agents with human organic anion transporting polypeptides. Antimicrob Agents Chemother. 2014 Aug;58(8):4555-64. [4]. Seung-Hoon Lee, et al. HA1077 displays synergistic activity with daclatasvir against hepatitis C virus and suppresses the emergence of NS5A resistance-associated substitutions in mice. Sci Rep. 2018 Aug 20;8(1):12469. |
Daclatasvir
CAS: 1009119-64-5 F: C40H50N8O6 W: 738.88
Daclatasvir (BMS-790052) is a potent and orally active HCV NS5A protein inhibitor with EC50s range of 9-146 pM for multi
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