Daclatasvir

Research use only, not for human use.

A potent HCV NS5A inhibitor with EC50 of <50 pM against genotype 1 replicons.

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