Reldesemtiv

1345410-31-2

384.38

DMSO : 250 mg/mL (650.40 mM; Need ultrasonic)

Others

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 uM. Reldesemtiv increases exercise performance in a heart failure model^[1]. In Vitro: Reldesemtiv selectively binds to and sensitizes the fast skeletal troponin complex to calcium^[1]. In Vivo: 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].