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MedKoo Cat#: 319737 | Name: Tirasemtiv
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

Tirasemtiv, also known as CK2017357, is a novel skeletal muscle activator or Troponin Activator. Tirasemtiv slows the rate of calcium release from troponin, thus sensitizing fast skeletal muscle fibers to calcium. Tirasemtiv demonstrated increases in skeletal muscle force in response to neuronal input and delays in the onset and reductions in the degree of muscle fatigue.

Chemical Structure

Tirasemtiv
Tirasemtiv
CAS#1005491-05-3

Theoretical Analysis

MedKoo Cat#: 319737

Name: Tirasemtiv

CAS#: 1005491-05-3

Chemical Formula: C12H14N4O

Exact Mass: 230.1168

Molecular Weight: 230.27

Elemental Analysis: C, 62.59; H, 6.13; N, 24.33; O, 6.95

Price and Availability

Size Price Availability Quantity
100mg USD 450.00 2 Weeks
200mg USD 750.00 2 Weeks
500mg USD 1,450.00 2 Weeks
1g USD 2,450.00 2 Weeks
2g USD 3,850.00 2 Weeks
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Related CAS #
1005491-05-3
Synonym
CK2017357; CK-2017357; CK 2017357; Tirasemtiv
IUPAC/Chemical Name
1-(1-Ethylpropyl)-6-ethynyl-1,3-dihydro-2H-imidazo(4,5-b)pyrazin-2-one
InChi Key
RSQGZEAXODVTOL-UHFFFAOYSA-N
InChi Code
InChI=1S/C12H14N4O/c1-4-8-7-13-10-11(14-8)16(12(17)15-10)9(5-2)6-3/h1,7,9H,5-6H2,2-3H3,(H,13,15,17)
SMILES Code
O=C1N(C(CC)CC)C2=NC(C#C)=CN=C2N1
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO, not in water
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info

Preparing Stock Solutions

The following data is based on the product molecular weight 230.27 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
1: Sanders DB, Rosenfeld J, Dimachkie MM, Meng L, Malik FI; Tirasemtiv in Myasthenia Gravis Study Group. 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. doi: 10.1007/s13311-015-0345-y. PubMed PMID: 25742919; PubMed Central PMCID: PMC4404445. 2: Bauer TA, Wolff AA, Hirsch AT, Meng LL, Rogers K, Malik FI, Hiatt WR. Effect of tirasemtiv, a selective activator of the fast skeletal muscle troponin complex, in patients with peripheral artery disease. Vasc Med. 2014 May 28;19(4):297-306. [Epub ahead of print] PubMed PMID: 24872402. 3: Hwee DT, Kennedy A, Ryans J, Russell AJ, Jia Z, Hinken AC, Morgans DJ, Malik FI, Jasper JR. 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. doi: 10.1371/journal.pone.0096921. eCollection 2014. PubMed PMID: 24805850; PubMed Central PMCID: PMC4013064. 4: Hansen R, Saikali KG, Chou W, Russell AJ, Chen MM, Vijayakumar V, Stoltz RR, Baudry S, Enoka RM, Morgans DJ, Wolff AA, Malik FI. Tirasemtiv amplifies skeletal muscle response to nerve activation in humans. Muscle Nerve. 2014 Dec;50(6):925-31. doi: 10.1002/mus.24239. PubMed PMID: 24634285; PubMed Central PMCID: PMC4260123. 5: Shefner JM, Watson ML, Meng L, Wolff AA; Neals/Cytokinetics STUDY Team. A study to evaluate safety and tolerability of repeated doses of tirasemtiv in patients with amyotrophic lateral sclerosis. Amyotroph Lateral Scler Frontotemporal Degener. 2013 Dec;14(7-8):574-81. doi: 10.3109/21678421.2013.822517. Epub 2013 Aug 19. PubMed PMID: 23952636. 6: Shefner JM, Wolff AA, Meng L. The relationship between tirasemtiv serum concentration and functional outcomes in patients with ALS. Amyotroph Lateral Scler Frontotemporal Degener. 2013 Dec;14(7-8):582-5. doi: 10.3109/21678421.2013.817587. Epub 2013 Aug 19. PubMed PMID: 23952600. 7: Miciak JJ, Warsing LC, Tibbs ME, Jasper JR, Jampel SB, Malik FI, Tankersley C, Wagner KR. Fast skeletal muscle troponin activator in the dy2J muscular dystrophy model. Muscle Nerve. 2013 Aug;48(2):279-85. doi: 10.1002/mus.23848. Epub 2013 Jun 29. PubMed PMID: 23512724. 8: Gibson SB, Bromberg MB. Amyotrophic lateral sclerosis: drug therapy from the bench to the bedside. Semin Neurol. 2012 Jul;32(3):173-8. doi: 10.1055/s-0032-1329193. Epub 2012 Nov 1. Review. PubMed PMID: 23117941. 9: Shefner J, Cedarbaum JM, Cudkowicz ME, Maragakis N, Lee J, Jones D, Watson ML, Mahoney K, Chen M, Saikali K, Mao J, Russell AJ, Hansen RL, Malik F, Wolff AA; Neals/Cytokinetics Study Team. Safety, tolerability and pharmacodynamics of a skeletal muscle activator in amyotrophic lateral sclerosis. Amyotroph Lateral Scler. 2012 Sep;13(5):430-8. doi: 10.3109/17482968.2012.684214. Epub 2012 May 16. PubMed PMID: 22591195. 10: Russell AJ, Hartman JJ, Hinken AC, Muci AR, Kawas R, Driscoll L, Godinez G, Lee KH, Marquez D, Browne WF 4th, Chen MM, Clarke D, Collibee SE, Garard M, Hansen R, Jia Z, Lu PP, Rodriguez H, Saikali KG, Schaletzky J, Vijayakumar V, Albertus DL, Claflin DR, Morgans DJ, Morgan BP, Malik FI. Activation of fast skeletal muscle troponin as a potential therapeutic approach for treating neuromuscular diseases. Nat Med. 2012 Feb 19;18(3):452-5. doi: 10.1038/nm.2618. PubMed PMID: 22344294; PubMed Central PMCID: PMC3296825. 11: von Haehling S, Stepney R, Anker SD. Advances in understanding and treating cardiac cachexia: highlights from the 5th Cachexia Conference. Int J Cardiol. 2010 Oct 29;144(3):347-9. doi: 10.1016/j.ijcard.2010.05.042. Epub 2010 Jun 19. PubMed PMID: 20561693.