Reldesemtiv(CK-2127107)是一种选择性的，口服活性的下一代快速骨骼肌肌钙蛋白(fastskeletalmuscletroponin)激活剂(FSTA)。Reldesemtiv选择性激活快速骨骼肌原纤维，EC50为3.4μM。Reldesemtiv可提高心力衰竭模型的运动表现。
货号:ajcx31394
CAS:1345410-31-2
分子式:C19H18F2N6O
分子量：384.38
溶解度:N/A
纯度：98%
存储：Store at -20°C
库存：现货

Background:

Reldesemtiv (CK-2127107) is a selective, orally active and next-generation fast skeletal muscle troponin activator (FSTA). Reldesemtiv selectively activates fast skeletal myofibrils with an EC50 of 3.4 μM. Reldesemtiv increases exercise performance in a heart failure model[1].

Reldesemtiv selectively binds to and sensitizes the fast skeletal troponin complex to calcium[1].

Reldesemtiv (10 mg/kg; p.o.) significantly improves rotarod performance in exercise-intolerant LAD-HF rats[1].Reldesemtiv (10 mg/kg; i.v.) increases Ca2+ sensitivity in fast skeletal muscle fibers and increases muscle force in response to submaximal stimulation frequencies in LAD-HF rats[1].Reldesemtiv increases sarcomeric Ca2+ sensitivity in skinned LAD-HF skeletal fibers[1]. Animal Model: Female Sprague-Dawley rats (Sham and left anterior descending coronary artery (LAD) heart failure (LAD-HF))[1]

[1]. Hwee DT, et al. The small-molecule fast skeletal troponin activator, CK-2127107, improves exercise tolerance in a rat model of heart failure. J Pharmacol Exp Ther. 2015 Apr;353(1):159-68. [2]. Andrews JA, et al. CK-2127107 amplifies skeletal muscle response to nerve activation in humans. Muscle Nerve. 2018 May;57(5):729-734.