阿那匹韦 T4474

Product Introduction
Bioactivity


英文名: Asunaprevir

描述: Asunaprevir (BMS-650032) 是一种有口服活性的 HCV NS3 蛋白酶抑制剂，IC50值为 0.2 nM-3.5 nM。它也是 SARS-CoV-2 3CLpro 抑制剂。

细胞实验: Cytotoxicity is determined by incubating cells (3,000 to 10,000 cells/well) with serially diluted test compounds or DMSO for 5 days (MT-2 cells) or 4 days (all other cell types). Cell viability is quantitated using an MTS assay for MT-2 or a Cell-Titer Blue reagent assay for HEK-293, HuH-7, HepG2, and MRC5 cells, and 50% cytotoxic concentrations (CC50s) are calculated.

动物实验: Mice (n=9 per group; overnight fast) receive Asunaprevir (ASV) by oral gavage (5 mg/kg; a vehicle of PEG-400-ethanol, 9:1). Blood samples (-0.2 mL) are obtained by retro-orbital bleeding at 0.25, 0.5, 1, 3, 6, 8, and 24 h after dosing. Within each group, three animals are bled at 0.25, 3, and 24 h, three at 0.5 and 6 h, and three at 1 and 8 h, resulting in a composite pharmacokinetic profile. Livers and brains are also removed from mice at the terminal sampling points. Rats (n=3 per group; overnight fast) receive ASV (amorphous free acid) by oral gavage (3, 5, 10, and 15 mg/kg) in PEG-400-ethanol (9:1). Serial blood samples (-0.3 mL) are obtained from the jugular vein predosing (0 h) and at 0.25, 0.5, 0.75, 1, 2, 4, 6, 8, 24, and 48 h post dosing. To assess tissue exposure, rats are orally administered ASV (5 or 15 mg/kg, same vehicle as above), and blood, liver, and heart samples from two rats/group are obtained at 0.17, 0.5, 1, 2, 4, 6, 8, 24, 48, and 72 h after dosing.

体外活性: Asunaprevir 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[2]. 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)[3]. Asunaprevir, administered at single or multiple doses of 200 to 600 mg twice daily, is generally well tolerated, achieving rapid and substantial decreases in HCV RNA levels in subjects chronically infected with genotype 1 HCV[4].

体内活性: Asunaprevir (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[2].

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: H2O : Insoluble
Ethanol : 20 mg/mL
DMSO : 50 mg/mL (66.82 mM)


关键字: Asunaprevir | inhibit | HCV | BMS 650032 | SARS-CoV | HCV Protease | Hepatitis C virus | Inhibitor | SARS coronavirus | BMS650032

相关产品: HCV-IN-30 | NM107 | TMC647055 Choline Hydroxide Salt | Chlorcyclizine | BAY-43-9695 | Simeprevir | ITX5061 | VCH-916 free acid(1200133-34-1 free base) | Methyl 2-amino-5-bromobenzoate | Ruzasvir

相关库: Anti-Aging Compound Library | Drug Repurposing Compound Library | Anti-COVID-19 Compound Library | Approved Drug Library | Bioactive Compounds Library Max | Human Metabolite Library | Inhibitor Library | Highly Selective Inhibitor Library | Target-Focused Phenotypic Screening Library | Anti-Viral Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途