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Tirasemtiv CAS: 1005491-05-3

Category: Inhibitors
Product Name: Tirasemtiv
Cat No: I000090
CAS No: 1005491-05-3
Molecular Formula: C12H14N4O
Molecular Weight: 230.27
SMILES: O=C1N(C(CC)CC)C2=NC(C#C)=CN=C2N1
InChI: None
InChIKey: None
Solubility: DMSO: ≥ 52 mg/mL
Target: Troponin activator
CAS 1005491-05-3,Tirasemtiv
  • Description

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].

  • Spec

Appearance:Solid powder
Purity: > 98%

  • References


1:A randomized, placebo-controlled, double-blind phase IIb trial evaluating the safety and efficacy of tirasemtiv in patients with amyotrophic lateral sclerosis. Shefner JM, Wolff AA, Meng L, Bian A, Lee J, Barragan D, Andrews JA; ; ON BEHALF OF THE BENEFIT-ALS STUDY GROUP..Amyotroph Lateral Scler Frontotemporal Degener. 2016 Jul-Aug;17(5-6):426-35. doi: 10.3109/21678421.2016.1148169. Epub 2016 Mar 16. PMID: 26982815
2: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. Sanders DB, Rosenfeld J, Dimachkie MM, Meng L, Malik FI; Tirasemtiv in Myasthenia Gravis Study Group..Neurotherapeutics. 2015 Apr;12(2):455-60. doi: 10.1007/s13311-015-0345-y. PMID: 25742919 Free PMC Article
3:Effect of tirasemtiv, a selective activator of the fast skeletal muscle troponin complex, in patients with peripheral artery disease. Bauer TA, Wolff AA, Hirsch AT, Meng LL, Rogers K, Malik FI, Hiatt WR.Vasc Med. 2014 Aug;19(4):297-306. Epub 2014 May 28. PMID: 24872402
4:Fast skeletal muscle troponin activator tirasemtiv increases muscle function and performance in the B6SJL-SOD1G93A ALS mouse model. Hwee DT, Kennedy A, Ryans J, Russell AJ, Jia Z, Hinken AC, Morgans DJ, Malik FI, Jasper JR.PLoS One. 2014 May 7;9(5):e96921. doi: 10.1371/journal.pone.0096921. eCollection 2014. PMID: 24805850 Free PMC Article
5:Tirasemtiv amplifies skeletal muscle response to nerve activation in humans. Hansen R, Saikali KG, Chou W, Russell AJ, Chen MM, Vijayakumar V, Stoltz RR, Baudry S, Enoka RM, Morgans DJ, Wolff AA, Malik FI.Muscle Nerve. 2014 Dec;50(6):925-31. doi: 10.1002/mus.24239. PMID: 24634285 Free PMC Article
6:A study to evaluate safety and tolerability of repeated doses of tirasemtiv in patients with amyotrophic lateral sclerosis. Shefner JM, Watson ML, Meng L, Wolff AA; Neals/Cytokinetics STUDY Team..Amyotroph Lateral Scler Frontotemporal Degener. 2013 Dec;14(7-8):574-81. doi: 10.3109/21678421.2013.822517. Epub 2013 Aug 19. PMID: 23952636
7:The relationship between tirasemtiv serum concentration and functional outcomes in patients with ALS. Shefner JM, Wolff AA, Meng L.Amyotroph Lateral Scler Frontotemporal Degener. 2013 Dec;14(7-8):582-5. doi: 10.3109/21678421.2013.817587. Epub 2013 Aug 19. PMID: 23952600


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