| 产品描述: | HCV 蛋白酶抑制剂;HCV Protease Inhibitors;;InformationDaclatasvir Dihydrochloride Daclatasvir is an orally available antiviral agent that inhibits the NS5A region of the hepatitis C virus (HCV) used for the treatment of chronic HCV genotype 1 and 3 infection.TargetsNS5AIn vitroDaclatasvir exhibited potent inhibition in all of the wild-type replicons and hybrid replicons representing the range of genotypes and subtypes. daclatasvir induces an alteration in the subcellular localization of NS5A, which inhibits the formation and activation of HCV RCs. Daclatasvir was found to have a high potency across all HCV genotypes with half-maximum effective concentrations (EC50) ranging from 9 to 146 pM. While it is pangenotypic, it has a low barrier to resistance against the subtype of Genotype 1a.In vivoDaclatasvir has good bioavailability in rats, dogs and cynomolgus monkey (F%= 50, 108 and 38 respectively). |
| 靶点: |
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) |
| 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. |
| 保存条件: |
-80℃(运输条件:冰袋低温运输) |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
1.232 ml |
6.159 ml |
12.318 ml |
| 5 mM |
0.246 ml |
1.232 ml |
2.464 ml |
| 10 mM |
0.123 ml |
0.616 ml |
1.232 ml |
| 50 mM |
0.025 ml |
0.123 ml |
0.246 ml |
|
| 注意: |
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