Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 389 | 现货 | ||
2 mg | ¥ 622 | 现货 | ||
5 mg | ¥ 1,330 | 现货 | ||
10 mg | ¥ 2,120 | 现货 | ||
25 mg | ¥ 3,890 | 现货 | ||
50 mg | ¥ 5,560 | 现货 | ||
100 mg | ¥ 7,790 | 现货 | ||
500 mg | ¥ 15,500 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,680 | 现货 |
产品描述 | Asunaprevir (BMS-650032) is an effective hepatitis C virus (HCV) NS3 protease inhibitor. |
靶点活性 | 4a (ED43):1.6 nM, 1b J4L6S:0.3 nM, 6a (HK-6A):0.9 nM, HCV 1a H77:0.7 nM, 5a (SA13):1.7 nM |
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]. |
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. |
别名 | BMS-650032, 阿那匹韦 |
分子量 | 748.29 |
分子式 | C35H46ClN5O9S |
CAS No. | 630420-16-5 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: Insoluble
Ethanol: 20 mg/mL
DMSO: 50 mg/mL (66.82 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 1.3364 mL | 6.6819 mL | 13.3638 mL | 33.4095 mL |
5 mM | 0.2673 mL | 1.3364 mL | 2.6728 mL | 6.6819 mL | |
10 mM | 0.1336 mL | 0.6682 mL | 1.3364 mL | 3.341 mL | |
20 mM | 0.0668 mL | 0.3341 mL | 0.6682 mL | 1.6705 mL | |
50 mM | 0.0267 mL | 0.1336 mL | 0.2673 mL | 0.6682 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Asunaprevir 630420-16-5 Microbiology/Virology Proteases/Proteasome HCV Protease SARS-CoV inhibit HCV BMS-650032 BMS 650032 Hepatitis C virus Inhibitor SARS coronavirus 阿那匹韦 BMS650032 inhibitor