Tirasemtiv 是一种快速骨骼肌型肌钙蛋白复合物激活剂。

Tirasemtiv is an activator of the fast skeletal muscle troponin complex.

Solid

Troponin

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 (Ca), and slows the rate of Ca release from the regulatory troponin complex of fast skeletal muscle. has not independently confirmed the accuracy of these methods. They are for reference only.

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) of ALS with functional deficits. Additionally, diaphragm force and tidal volume are significantly higher in Tirasemtiv-treated female B6SJL-SOD1 mice. At the 25% deficit milestone, vehicle-treated B6SJL-SOD1 mice demonstrated forelimb grip strength of 49.6±4.6 g. Tirasemtiv increases grip strength by 38% to 68.6±8.1g (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 mice (WT p<0.0001; mid-stage p=0.0028). At later stages of di

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[1]. Hwee DT, et al. Fast skeletal muscle troponin activator tirasemtiv increases muscle function and performance in the B6SJL-SOD1G93A ALS mouse model. PLoS One. 2014 May 7;9(5):e96921.

In Vitro: DMSO : 10.91 mg/mL (47.38 mM; Need ultrasonic)配制储备液