Powder: -20°C for 3 years | In solvent: -80°C for 1 year
PF-4981517 (CYP3cide) 是一种高效,特异性和时间依赖性细胞色素P4503A4 (CYP3A4)抑制剂。对于CYP3A4,CYP3A5 和 CYP3A7,抑制CYP3A 活性的IC50值分别为 0.03 μM,17 μM 和 71μM。PF-4981517 可用于区分CYP3A4和 CYP3A5 对于药物代谢的作用。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 369 | 现货 | ||
5 mg | ¥ 828 | 现货 | ||
10 mg | ¥ 1,330 | 现货 | ||
25 mg | ¥ 2,820 | 现货 | ||
50 mg | ¥ 4,250 | 现货 |
产品描述 | PF-4981517 (CYP3cide) is a efficient, specific and time-dependent inhibitor of cytochrome P4503A4 (CYP3A4). The IC 50 values for CYP3A activity are 0.03 μM,17 μM, and 71 μM for CYP3A4, CYP3A5, and CYP3A7, respectively. PF-4981517 is able to be used to distinguish the contributions of CYP3A4 versus CYP3A5 on drug Metabolism. |
体外活性 | When investigating the inhibition of CYP3cide, an extreme metabolic inactivation efficiency (k inact /K I ) of 3300 to 3800 ml min -1 μmol -1 is observed in human liver microsomes from donors of nonfunctioning CYP3A5 (CYP3A5 * 3/ * 3). This observed efficiency equated to an apparent KI between 420 and 480 nM with a maximal inactivation rate (kinact) equal to 1.6 min -1. When CYP3cide is tested at a concentration and preincubation time to completely inhibit CYP3A4 in a library of genotyped polymorphic CYP3A5 microsomes, the correlation of the remaining CYP3A activity to CYP3A5 abundance is significant. |
别名 | CYP3cide |
分子量 | 456.59 |
分子式 | C26H32N8 |
CAS No. | 1390637-82-7 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 9 mg/mL (19.7 mM), Sonication and heating to 60℃ are recommended.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.1901 mL | 10.9507 mL | 21.9015 mL | 54.7537 mL |
5 mM | 0.438 mL | 2.1901 mL | 4.3803 mL | 10.9507 mL | |
10 mM | 0.219 mL | 1.0951 mL | 2.1901 mL | 5.4754 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。
PF-4981517 1390637-82-7 Metabolism P450 PF 4981517 PF4981517 CYP3cide Inhibitor inhibitor inhibit