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Tirasemtiv is an activator of the fast skeletal muscle troponin complex that sensitizes the sarcomere to Ca2+ and increases muscle force. Tirasemtiv displays neuromodulatory activity; it improves motor functions in models of amyotrophic lateral sclerosis (ALS) and is currently in clinical trials as a potential treatment for myasthenia gravis and other neurodegenerative diseases.
| Cas No. | 1005491-05-3 |
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| Purity | ≥99% |
| Formula | C12H14N4O |
| Formula Wt. | 230.27 |
| IUPAC Name | 6-Ethynyl-1-(3-pentanyl)-1,3-dihydro-2H-imidazo[4,5-b]pyrazin-2-one |
| Synonym | CK-2017357, Troponin Activator |
| Solubility | DMSO: ≥ 52 mg/mL |
| Store Temp | -20°C |
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| Ship Temp | Ambient |
| MSDS | |
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| Info Sheet |
Sanders DB, Rosenfeld J, Dimachkie MM, et al. A Double-Blinded, Randomized, Placebo-Controlled Trial to Evaluate Efficacy, Safety, and Tolerability of Single Doses of Tirasemtiv in Patients with Acetylcholine Receptor-Binding Antibody-Positive Myasthenia Gravis. Neurotherapeutics. 2015 Apr;12(2):455-60. PMID: 25742919.
Hwee DT, Kennedy A, Ryans J, et al. Fast skeletal muscle troponin activator tirasemtiv increases muscle function and performance in the B6SJL-SOD1G93A ALS mouse model. PLoS One. 2014 May 7;9(5):e96921. PMID: 24805850.
Russell AJ, Hartman JJ, Hinken AC, et al. Activation of fast skeletal muscle troponin as a potential therapeutic approach for treating neuromuscular diseases. Nat Med. 2012 Feb 19;18(3):452-5. PMID: 22344294.