Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Clomethiazole (Distraneurin) 是口服GABAA 激动剂,可抑制人肝微粒体中的细胞色素 P450 异构体,CYP2A6 和 CYP2E1。它有抗惊厥作用,具有治疗惊厥性癫痫持续状态的潜力。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
50 mg | ¥ 298 | 现货 | ||
100 mg | ¥ 418 | 现货 | ||
500 mg | ¥ 997 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 460 | 现货 |
产品描述 | Clomethiazole (Distraneurin) is an orally active GABAA agonist and it is an anticonvulsant agent. It also has the potential for treating convulsive status epilepticus. Chlormethiazole inhibits cytochrome P450 isoforms: CYP2A6 and CYP2E1 in human liver microsomes. |
靶点活性 | CYP2A6/CYP2E1:24 µM and 42 µM |
体外活性 | Clomethiazole inhibits cytochrome P450 isoforms, CYP2A6 and CYP2E1 (IC50: 24 μM and 42 μ), in human liver microsomes. But all other isoforms exhibiting values > 300 μM[2]. Clomethiazole (1 mM), in the absence of GABA, to α1/β1/γ2 or α1/β2/γ2 subunit-containing cells produced large whole-cell currents[1]. Clomethiazole activate GABAA currents in α1/β1/γ2- and α1/β2/γ2-containing cells ( EC50: 0.3 and 1.5 mM) [1]. Clomethiazole (30 μM) at low concentration also potentiates the action of GABA in both cell types, equivalent to a 3-fold increase in potency and up to 1.8-fold increase in maximal current[1]. |
别名 | Distraneurin, Chlormethiazole, 氯美噻唑, 5-(2-CHLOROETHYL)-4-METHYLTHIAZOLE |
分子量 | 161.65 |
分子式 | C6H8ClNS |
CAS No. | 533-45-9 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 240 mg/mL (1484.69 mM), Sonication is recommended.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 6.1862 mL | 30.931 mL | 61.862 mL | 154.6551 mL |
5 mM | 1.2372 mL | 6.1862 mL | 12.3724 mL | 30.931 mL | |
10 mM | 0.6186 mL | 3.0931 mL | 6.1862 mL | 15.4655 mL | |
20 mM | 0.3093 mL | 1.5466 mL | 3.0931 mL | 7.7328 mL | |
50 mM | 0.1237 mL | 0.6186 mL | 1.2372 mL | 3.0931 mL | |
100 mM | 0.0619 mL | 0.3093 mL | 0.6186 mL | 1.5466 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。
Clomethiazole 533-45-9 Membrane transporter/Ion channel Metabolism Neuroscience P450 GABA Receptor inhibit Distraneurin Cytochrome P450 sedative anticonvulsant Gamma-aminobutyric acid Receptor Chlormethiazole alcoholism insomnia CYPs Inhibitor neuroprotective γ-Aminobutyric acid Receptor 氯美噻唑 5-(2-CHLOROETHYL)-4-METHYLTHIAZOLE inhibitor