Synonyms: CK-2017357
Compound class:
Synthetic organic
Comment: Tirasemtiv acts as an activator of the fast skeletal muscle (type II) troponin complex [4]. The compound is being investigated as a potential treatment for diseases and conditions associated with aging, muscle weakness and wasting or neuromuscular dysfunction [4] (e.g. amyotrophic lateral sclerosis [5], myasthenia gravis and claudication [2]). In clinical trial tirasemtiv was not well tolerated, and this was likely a contributory factor to its lack of significant efficacy.
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Bioactivity Comments |
Tirasemtiv interacts directly with fast skeletal troponin isolated from rabbit psoas with a Kd of 40nM [4]. Experimental results suggest that the binding site for tirasemtiv is formed at an interface between two or more troponin subunits [4]. No publicly available affinity data for the human target is available. |