Tirasemtiv(CK-2017357) tiraseMtiv (CK-2017357);6-ethynyl-1-(pentan-3-yl)-1H-iMidazo[4,5-b]pyrazin-2-ol;TiraseMtiv;1-(1-Ethylpropyl)-6-ethynyl-1,3-dihydro-2H-imidazo[4,5-b]pyrazin-2-one;CK 2017357;Tirasemtiv 1-(1-Ethylpropyl 1005491-05-3
Tirasemtiv(CK 2017357) is a a small-molecule fast-skeletal-troponin activator, which is being developed as a potential treatment for diseases and conditions associated with aging, muscle weakness and wasting or neuromuscular dysfunction.
IC50 value:
Target: Troponin activator
Binding selectively to the fast-skeletal-troponin complex, CK-2017357 slows the rate of calcium release from troponin C and sensitizes muscle to calcium. CK-2017357 increases the production of muscle force in situ at sub-maximal nerve stimulation rates. sensitization of the fast-skeletal-troponin complex to calcium improves muscle force and grip strength immediately after administration of single doses of CK-2017357 in a model of the neuromuscular disease myasthenia gravis [1]. single doses of 250 mg and 500 mg of CK-2017357 were safe and well tolerated by patients with ALS [2]. Mice receiving a high dose of tirasemtiv had significantly higher muscle fiber cross-sectional area and respiratory response to CO stimulation at 16 weeks than mice on low dose or placebo [3].
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