Powder: -20°C for 3 years | In solvent: -80°C for 1 year
BTK inhibitor 17 是口服有效的、不可逆的BTK 抑制剂,IC50为 2.1 nM。BTK inhibitor 17在类风湿关节炎方面有研究的价值。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 1,380 | 现货 | ||
5 mg | ¥ 3,690 | 现货 | ||
10 mg | ¥ 5,320 | 现货 | ||
25 mg | ¥ 8,250 | 现货 | ||
50 mg | ¥ 10,900 | 现货 | ||
100 mg | ¥ 14,800 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 3,690 | 现货 |
产品描述 | BTK inhibitor 17 is a potent irreversible BTK inhibitor (IC50 = 2.1 nM). BTK inhibitor 17 can be used in rheumatoid arthritis studies. |
靶点活性 | BTK:2.1 nM |
体外活性 | BTK inhibitor 17 exhibited high potency against BTK kinase and acceptable PK profile. BTK inhibitor 17 could covalently bind to Cys481 and formed an HB network with gatekeeper Thr474, hinge key residues Met477 and Glu475[1]. |
体内活性 | BTK inhibitor 17 demonstrated significant in vivo efficacy in a mouse-collagen-induced arthritis (CIA) model. BTK inhibitor 17 shows >95% plasma protein binding across three species of human, rat, and mouse. After an intravenous injection, the half-life (rat, 0.32 h; mice, 0.42 h), clearance (rat, 54.6 mL/min/kg; mice, 31.3 mL/min/kg), volume of distribution (rat, 1.55 L/kg; mice, 0.82 L/kg), and AUC exposure (rat, 604 ng.h/mL; mice, 576 ng.h/mL) are observed in two species. After oral administration, BTK inhibitor 17 exhibits higher Cmax (rat, 466 ng/mL; mice, 252 ng/mL) and plasma exposure (rat, 642 ng.h/mL; mice, 128 ng.h/mL) with a favorable oral bioavailability (rat, 23.7%; mice, 11.2%)[1]. In male Balb/C mice injected with collagen, BTK inhibitor 17 inhibited the significant progression of the disease and exhibited a clear dose-dependent reduction per paw clinical scores[1]. |
分子量 | 456.5 |
分子式 | C25H24N6O3 |
CAS No. | 1858206-76-4 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 100 mg/mL (219.06 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.1906 mL | 10.9529 mL | 21.9058 mL | 54.7645 mL |
5 mM | 0.4381 mL | 2.1906 mL | 4.3812 mL | 10.9529 mL | |
10 mM | 0.2191 mL | 1.0953 mL | 2.1906 mL | 5.4765 mL | |
20 mM | 0.1095 mL | 0.5476 mL | 1.0953 mL | 2.7382 mL | |
50 mM | 0.0438 mL | 0.2191 mL | 0.4381 mL | 1.0953 mL | |
100 mM | 0.0219 mL | 0.1095 mL | 0.2191 mL | 0.5476 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。
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