Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Grazoprevir (MK-5172) 是一种丙型肝炎病毒 NS3/4a 蛋白酶的选择性抑制剂,具有跨基因型和耐药变体的广泛活性,对 gt1b、gt1a、gt2a、gt2b 和 gt3a 的Ki 分别为 0.01 nM、0.01 nM、0.08 nM、0.15 nM 和 0.90 nM。它也是 SARS-CoV-2 3CLpro 抑制剂。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 645 | 现货 | ||
2 mg | ¥ 1,060 | 现货 | ||
5 mg | ¥ 1,980 | 现货 | ||
10 mg | ¥ 3,350 | 现货 | ||
25 mg | ¥ 5,880 | 现货 | ||
50 mg | ¥ 8,290 | 现货 | ||
100 mg | ¥ 10,900 | 现货 | ||
500 mg | ¥ 22,300 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 3,130 | 现货 |
产品描述 | Grazoprevir (MK-5172) is a selective inhibitor of Hepatitis C virus NS3/4a protease with broad activity across genotypes and resistant variants, with Ki of 0.01 nM (gt1a), 0.08 nM (gt2a), 0.90 nM (gt3a), 0.01 nM (gt1b), 0.15 nM (gt2b), respectively. |
靶点活性 | GT1a:0.01 nM (Ki), GT1b:0.01 nM (Ki), GT2a:0.08 nM (Ki), GT2b:0.15 nM (Ki), GT3a:0.90 nM (Ki) |
体外活性 | In biochemical assays, MK-5172 is effective against a panel of major genotypes and variants engineered with common resistant mutations, with Ki of 0.01 nM (gt1b), 0.01 nM (gt1a), 0.08 nM (gt2a), 0.15 nM (gt2b), 0.90 nM (gt3a), 0.07 nM (gt1bR155K), 0.14 nM (gt1bD168V), 0.30 nM (gt1bD168Y), 5.3 nM (gt1bA156T), and 12 nM (gt1bA156V), respectively. In the replicon assay, MK-5172 demonstrates subnanomolar to low-nanomolar EC50s against genotypes 1a, 1b, and 2a, with EC50s of 0.5±0.1 nM, 2±1 nM, and 2±1 nM for gt1bcon1, gt1a, and gt2a, respectively. MK-5172 is potent against a panel of HCV replication mutants NS5A (Y93H) (EC50: 0.7 nM), NS5B nucleosides (S282T) (EC50: 0.3 nM), and NS5B (C316Y) (EC50: 0.4 nM)[1]. MK-5172 maintains the excellent potency against the gt 3a enzyme as well as a broad panel of mutant enzymes, has excellent potency in the replicon system [gt1b IC50(50% NHS): 7.4 nM; gt1a IC50(40% NHS): 7 nM], and shows excellent rat liver exposure[2]. |
体内活性 | When dosed to dogs, MK-5172 shows low clearance of 5 mL/min/kg and a 3 h half-life after iv dosing and has good plasma exposure (AUC: 0.4 μM/h) after a 1 mg/kg oral dose. Dog liver biopsy studies showed that the liver concentration of MK-5172 after the 1 mg/kg oral dose is 1.4 μM at the 24 h time point. Similar to its behaviour in rats, MK-5172 demonstrates effective partitioning into liver tissue and maintains high liver concentration, relative to potency, 24 h after oral dosing in dogs [2]. |
别名 | MK-5172 |
分子量 | 766.9 |
分子式 | C38H50N6O9S |
CAS No. | 1350514-68-9 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 55 mg/mL (71.72 mM)
Ethanol: 15 mg/mL
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 1.304 mL | 6.5198 mL | 13.0395 mL | 32.5988 mL |
5 mM | 0.2608 mL | 1.304 mL | 2.6079 mL | 6.5198 mL | |
10 mM | 0.1304 mL | 0.652 mL | 1.304 mL | 3.2599 mL | |
20 mM | 0.0652 mL | 0.326 mL | 0.652 mL | 1.6299 mL | |
50 mM | 0.0261 mL | 0.1304 mL | 0.2608 mL | 0.652 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。
Grazoprevir 1350514-68-9 Microbiology/Virology Proteases/Proteasome HCV Protease SARS-CoV Hepatitis C virus MK5172 HCV Inhibitor inhibit MK 5172 MK-5172 SARS coronavirus inhibitor