Daclatasvir dihydrochloride

SKU: orb1227165

Description

A potent HCV NS5A inhibitor with EC50 of <50 pM against genotype 1 replicons; exhibits picomolar EC(50) towards replicons expressing a broad range of HCV genotypes and the JFH-1 genotype 2a infectious virus in cell culture.HCV Infection Approved(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). Daclatasvir (BMS-790052) binds tightly to NS5A33-202 and NS5A26-202 with Kds of 8 nM and 210 nM, respectively.(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.

Key Properties

• CAS Number: 1009119-65-6
• MW: 811.7969
• Purity: >98% (HPLC)
• Formula: C₄₀H₅₂Cl₂N₈O₆
• SMILES: CC(C)[C@@H](C(=O)N1CCC[C@H]1C2=NC=C(N2)C3=CC=C(C=C3)C4=CC=C(C=C4)C5=CN=C(N5)[C@@H]6CCCN6C(=O)[C@H](C(C)C)NC(=O)OC)NC(=O)OC.Cl.Cl
• Target: HCV
• Solubility: DMSO: ≥ 56 mg/mL

Bioactivity

• 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. Animal model: NOD/SCID male mice (5 weeks of age, 18-20 g) bearing HCV RNA-transfected cells. Dosage: 30 mg/kg. Administration: Oral administration; daily; for 27 days. Result: Reduced serum HCV RNA titers very rapidly by ~1.5 log10 at day 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). Daclatasvir (BMS-790052) binds tightly to NS5A33-202 and NS5A26-202 with Kds of 8 nM and 210 nM, respectively.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

BMS-790052 dihydrochloride | BMS790052 dihydrochloride | BMS 790052 dihydrochloride

Quick Database Links

Gene Symbol

HCV