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BMS-790052

Cat. No. M1843
BMS-790052 Structure
Synonym:

Daclatasvir; EBP 883

Size Price Availability Quantity
5mg USD 50  USD50 In stock
10mg USD 73  USD73 In stock
25mg USD 155  USD155 In stock
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Quality Control & Documentation
Biological Activity

BMS-790052 is a first-in-class, nonstructural protein 5A (NS5A) replication complex inhibitor with an EC50 of 9-50 pM. It is one of the most potent inhibitors of HCV replication reported so far. BMS-790052 inhibits hybrid replicons containing HCV genotype-4 NS5A genes with EC50 of 7–13 pM. Residue 30 of NS5A is an important site for BMS-790052-mediated resistance in the hybrid replicons. BMS-790052 was well tolerated in all dose groups, with adverse events occurring with a similar frequency in BMS-790052- and placebo-treated groups. BMS-7590052 is the first NS5A replication complex inhibitor with multiple dose proof-of-concept in clinic. At doses of 1-100 mg daily, BMS-790052 was well tolerated, had a PK profile supportive of once-daily dosing, and produced a rapid and substantial decrease in HCV-RNA levels in patients chronically infected with HCV genotype 1.

Chemical Information
Molecular Weight 738.88
Formula C40H50N8O6
CAS Number 1009119-64-5
Solubility (25°C) DMSO ≥40 mg/mL
Ethanol ≥40 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Pelosi et al. Antimicrob Agents Chemother. Effect on HCV Replication by Combinations of Direct Acting Antivirals Including NS5A Inhibitor Daclatasvir.

[2] Lim et al. J Biol Chem. Correlation between NS5A Dimerization and Hepatitis C Virus Replication.

[3] Kumthip et al. J Virol. Hepatitis C Virus NS5A Disrupts STAT1 Phosphorylation and Suppresses Type I Interferon Signaling.

[4] Suzuki et al. J Clin Virol. Prevalence of hepatitis C virus variants resistant to NS3 protease inhibitors or the NS5A inhibitor (BMS-790052) in hepatitis patients with genotype 1b.

[5] Jiang et al. J Chromatogr A. A sensitive and accurate liquid chromatography-tandem mass spectrometry method for quantitative determination of the novel hepatitis C NS5A inhibitor BMS-790052 (daclastasvir) in human plasma and urine.

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Keywords: BMS-790052, Daclatasvir; EBP 883 supplier, HCV Protease, inhibitors, activators


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