Synonyms: CK-107 | CK-2127107 | CK2127107
Compound class:
Synthetic organic
Comment: Reldesemtiv (CK-2127107) is a second generation fast skeletal muscle troponin activator [1], that was designed to improve upon tirasemtiv. Reldesemtiv slows the rate of calcium release from the troponin complex, and sensitises the sarcomere to calcium which leads to increased contractility in fast skeletal muscle fibres. Like tirasemtiv, reldesemtiv was proposed to offer a therapeutic option for debilitating muscle weakness/muscle fatigue in diseases such as spinal muscular atrophy (SMA) and amyotrophic lateral sclerosis (ALS).
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References |
1. Hwee DT, Kennedy AR, Hartman JJ, Ryans J, Durham N, Malik FI, Jasper JR. (2015)
The small-molecule fast skeletal troponin activator, CK-2127107, improves exercise tolerance in a rat model of heart failure. J Pharmacol Exp Ther, 353 (1): 159-68. [PMID:25678535] |
2. Shefner JM, Andrews JA, Genge A, Jackson C, Lechtzin N, Miller TM, Cockroft BM, Meng L, Wei J, Wolff AA et al.. (2021)
A Phase 2, Double-Blind, Randomized, Dose-Ranging Trial Of Reldesemtiv In Patients With ALS. Amyotroph Lateral Scler Frontotemporal Degener, 22 (3-4): 287-299. [PMID:32969758] |