Daclatasvir

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种有效的 HCV NS5A 抑制剂，针对基因型 1 复制子的 EC50 <50 pM。

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.

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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.

BMS-790052 | EBP 883 | BMS 790052

Microbiology/Virology

HCV

HCVNS5A

Infection

HCV Infection

1009119-64-5

738.875

C40H50N8O6

>98% (HPLC)

DMSO: ≥ 40 mg/mL

COC(=O)N[C@@H](C(C)C)C(=O)N1CCC[C@H]1C1=NC=C(N1)C1=CC=C(C=C1)C1=CC=C(C=C1)C1=CN=C(N1)[C@@H]1CCCN1C(=O)[C@@H](NC(=O)OC)C(C)C |r,c:19,25,27,32,34,39,t:17,23,30,37|

Carbamic acid, N,N'-[[1,1'-biphenyl]-4,4'-diylbis[1H-imidazole-5,2-diyl-(2S)-2,1-pyrrolidinediyl[(1S)-1-(1-methylethyl)-2-oxo-2,1-ethanediyl]]]bis-, C,C'-dimethyl ester

(-20℃)

With Ice Pack

≥ 2 years