Reldesemtiv

Reldesemtiv is an activator of fast skeletal troponin.¹ It increases ATPase activity in isolated rabbit psoas muscle myofibril preparations with a 40% activation concentration (AC₄₀) value of 0.6 µM. Reldesemtiv is selective for fast skeletal troponin over cardiac and slow skeletal troponin.² It is also selective for fast skeletal troponin over a panel of 79 enzymes, receptors, ion channels, and transporters at 100 µM.¹ Reldesemtiv increases muscle tension in a skinned fast skeletal muscle fiber assay with a 30% muscle force (DF30) value of 0.8 µM.¹ In vivo, reldesemtiv (10 mg/kg, p.o.) increases running time in the rotarod test, indicating increased exercise performance, in a rat model of heart failure-induced skeletal myopathy.²

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1. Collibee, S.E., Bergnes, G., Chuang, C., et al. Discovery of Reldesemtiv, a Fast Skeletal Muscle Troponin Activator for the Treatment of Impaired Muscle Function. J. Med. Chem. 64(2), 14930-14941 (2021).

2. Hwee, D.T., Kennedy, A.R., Hartman, J.J., 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. 353(1), 159-168 (2015).