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编 号:F004545
分子式:C40H52Cl2N8O6
分子量:811.8
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10mM*1mL in DMSO
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5mg
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10mg
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50mg
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100mg
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生物活性:
Daclatasvir dihydrochloride (BMS-790052 dihydrochloride) is a potent and orally active HCV NS5A protein inhibitor with EC50s range of 9-146 pM for multiple HCV replicon genotypes. Daclatasvir dihydrochloride is also an organic anion transporting polypeptide 1B (OATP1B) and OATP1B3 inhibitor with IC50s of 1.5 μM and 3.27 μM, respectively.

体内研究:
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.

体外研究:
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.
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