Reldesemtiv 是一种快速骨骼肌肌钙蛋白的选择性激活剂,EC50 为 3.4 μM。 Reldesemtiv 提高了心力衰竭模型中的运动表现。
产品描述
Reldesemtiv is a selective activator of fast skeletal muscle troponin with an EC50 of 3.4 μM. Reldesemtiv increases exercise performance in the heart failure model.
体外活性
Reldesemtiv selectively binds to the fast skeletal troponin complex and sensitizes to calcium [1].
体内活性
Reldesemtiv increases sarcomeric Ca2+ sensitivity in skinned LAD-HF skeletal fibers. In exercise-intolerant LAD-HF rats, Reldesemtiv (10 mg/kg; p.o.) obviously improves rotarod performance. Reldesemtiv (10 mg/kg; i.v.) enhances Ca2+ sensitivity in fast skeletal muscle fibers and increases muscle force in response to submaximal stimulation frequencies[1].
Cas No.
1345410-31-2
分子式
C19H18F2N6O
分子量
384.38
别名
CK-2127107;Reldesemtiv
储存和溶解度
DMSO:225mg/mL (585.4mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years