Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Tirasemtiv (CK-2017357) 是一种快速骨骼肌型肌钙蛋白复合物激活剂。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 343 | 现货 | ||
2 mg | ¥ 497 | 现货 | ||
5 mg | ¥ 822 | 现货 | ||
10 mg | ¥ 997 | 现货 | ||
25 mg | ¥ 1,990 | 现货 | ||
50 mg | ¥ 2,890 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 455 | 现货 |
产品描述 | Tirasemtiv (CK-2017357)(CK 2017357) is a small-molecule fast-skeletal-troponin activator, with a potential treatment for muscle weakness and neuromuscular dysfunction. |
体外活性 | Tirasemtiv is a fast skeletal troponin activator that sensitizes the sarcomere to calcium; this mechanism of action amplifies the response of muscle to neuromuscular input producing greater force when nerve input is reduced. Tirasemtiv selectively sensitizes fast skeletal muscle troponin to calcium (Ca2+), and slows the rate of Ca2+ release from the regulatory troponin complex of fast skeletal muscle[1]. |
体内活性 | A single dose of Tirasemtiv significantly increases submaximal isometric force, forelimb grip strength, grid hang time, and rotarod performance in a female transgenic mouse model (B6SJL-SOD1 g93A) of ALS with functional deficits. Additionally, diaphragm force and tidal volume are significantly higher in Tirasemtiv-treated female B6SJL-SOD1 g93A mice. At the 25% deficit milestone, vehicle-treated B6SJL-SOD1 g93A mice demonstrated forelimb grip strength of 49.6±4.6 g. Tirasemtiv increases grip strength by 38% to 68.6±8.1 g (p<0.05, single tailed t-test). Tirasemtiv doses of 2, 2, 2, and 4 mg/kg given at approximately 20 min intervals to achieve a cumulative dose of 10 mg/kg. Regression analysis of the log dose vs. response relationship indicated that Tirasemtiv significantly increased muscle force in WT and mid-stage B6SJL-SOD1 g93A mice (WT p<0.0001; mid-stage p=0.0028). At later stages of disease, the mice exhibited a trend for increased muscle function in response to Tirasemtivcompared to baseline (p=0.064)[1]. |
别名 | CK-2017357, 泰拉生替 |
分子量 | 230.27 |
分子式 | C12H14N4O |
CAS No. | 1005491-05-3 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 60 mg/mL (260.56 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 4.3427 mL | 21.7136 mL | 43.4273 mL | 108.5682 mL |
5 mM | 0.8685 mL | 4.3427 mL | 8.6855 mL | 21.7136 mL | |
10 mM | 0.4343 mL | 2.1714 mL | 4.3427 mL | 10.8568 mL | |
20 mM | 0.2171 mL | 1.0857 mL | 2.1714 mL | 5.4284 mL | |
50 mM | 0.0869 mL | 0.4343 mL | 0.8685 mL | 2.1714 mL | |
100 mM | 0.0434 mL | 0.2171 mL | 0.4343 mL | 1.0857 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。
Tirasemtiv 1005491-05-3 Others inhibit CK-2017357 泰拉生替 CK 2017357 CK2017357 Inhibitor inhibitor