Tirasemtiv (CK-2017357) 是一种直接快速骨骼肌钙蛋白激活剂,可以选择性结合快速骨骼肌钙蛋白,减缓钙释放速率,并使肌肉对钙敏感,可用于重症肌无力、间歇性跛行和肌萎缩侧索硬化的相关研究。
生物活性
Tirasemtiv (CK-2017357) slows the rate of calcium release from troponin C and sensitizes muscle to calcium. Tirasemtiv (CK-2017357) increases the production of muscle strength in situ at sub-maximal nerve stimulation rates. Single doses of 250 mg and 500 mg of Tirasemtiv were safe and well tolerated by patients with ALS. sensitization of the fast-skeletal-troponin complex to calcium improves muscle force and grip strength immediately after administration of single doses of Tirasemtiv in a model of the neuromuscular disease myasthenia gravis.
化学性质
分子量 | 230.27 |
分子式 | C12H14N4O |
CAS号 | 1005491-05-3 |
溶解性(25°C) | DMSO 10 mg/mL |
储存条件 | 粉末型式 -20°C 3年;4°C 2年 溶于溶剂 -80°C 6个月;-20°C 1个月 |
运输方式 | 冰袋运输,根据产品的不同,可能会有相应调整。 |
储备液配制
*下述溶液配置方法仅为基于分子量计算出的理论值。不同产品在配置溶液前,需考虑其在不同溶剂中的溶解度限制。
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 4.3427 mL | 21.7136 mL | 43.4273 mL |
5 mM | 0.8685 mL | 4.3427 mL | 8.6855 mL |
10 mM | 0.4343 mL | 2.1714 mL | 4.3427 mL |