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CAS No. : 630420-16-5
MCE 国际站:Asunaprevir
产品活性:Asunaprevir (BMS-650032) 是一种有效的,具有口服活性的 hepatitis C virus (HCV) NS3 protease 抑制剂,IC50 值为 0.2 nM-3.5 nM。Asunaprevir 抑制 SARS-CoV-2 3CLpro 活性。
研究领域:Anti-infection | Metabolic Enzyme/Protease
作用靶点:HCV | HCV Protease | SARS-CoV
In Vitro: In multiple experiments, populations of resistant colonies are markedly reduced when cells are treated with a combination of DCV and Asunaprevir.
Asunaprevir (ASV) inhibits the NS3 proteolytic activity of genotype 1a (H77 strain) and genotype 1b (J4L6S strain), with IC50s of 0.7 and 0.3 nM, respectively. The EC50s of ASV against replicons encoding the NS3 protease domains representing genotypes 1a, 1b, and 4a, range from 1.2 to 4.0 nM.
Replicon cells are maintained under selective pressure with asunaprevir at concentrations of 10 and 30 times the EC50 values (50 or 150 nM final concentrations, respectively). For genotype 1b resistance selection, replicon cells are maintained in the presence of asunaprevir at 10 or 30 times the EC50 values (30 or 90 nM final concentrations, respectively).
In Vivo: Asunaprevir (ASV, 3-15 mg/kg, p.o.) displays a hepatotropic disposition (liver-to-plasma ratios ranging from 40- to 359-fold across species) in several animal species. Twenty-four hours postdose, liver exposures across all species tested are ≥110-fold above the inhibitor EC50 observed with HCV genotype-1 replicons.
相关产品:Drug Repurposing Compound Library Plus | FDA-Approved Drug Library Plus | FDA-Approved Drug Library Mini | Bioactive Compound Library Plus | Anti-Infection Compound Library | Metabolism/Protease Compound Library | FDA-Approved Drug Library | Antiviral Compound Library | Drug Repurposing Compound Library | Anti-COVID-19 Compound Library | NMPA-Approved Drug Library | Orally Active Compound Library | FDA Approved & Pharmacopeial Drug Library | Anti-Hepatitis C Virus Compound Library | Targeted Diversity Library | Heterocyclic Compound Library | Sofosbuvir impurity J | Alisporivir | Antimicrobial agent-10 | GS-9256 | SARS-CoV-2-IN-23 | PSI-7409 tetrasodium | 3CPLro-IN-1 | Dasabuvir | FNC-TP | DDX3-IN-1 | SP inhibitor 1 | rel-Zotatifin | Monodes(N-carboxymethyl)valine Daclatasvir | Antioxidant agent-9 | Regdanvimab | Silymarin | NHC-triphosphate tetraammonium | Sofosbuvir-d6 | Grazoprevir potassium salt | Atazanavir | Daclatasvir-d16 | FWM-4 | Amantadine-d6 | Deferiprone | Ketotifen fumarate | Dehydrojuncusol | Daclatasvir dihydrochloride | SARS-CoV-2-IN-27 | Ribavirin | MMT5-14
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货号: HY-14434
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