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Product name : Tirasemtiv
Item : CR1815
Price : 100mg, $945; 200mg, $1485
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CAS : 1005491-05-3
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Details:
 Chemical Information
M.Wt 230.27 Storage Please store the product under the recommended conditions in the Certificate of Analysis.
Formula C12H14N4O
CAS No 1005491-05-3
Solubility

DMSO



Biological Activity of Tirasemtiv

 

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].

 

[1]. Russell AJ, 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.

[2]. Shefner J, et al. Safety, tolerability and pharmacodynamics of a skeletal muscle activator in amyotrophic lateral sclerosis. Amyotroph Lateral Scler. 2012 Sep;13(5):430-8.

[3]. Miciak JJ, et al. Fast skeletal muscle troponin activator in the dy2J muscular dystrophy model. Muscle Nerve. 2013 Aug;48(2):279-85.


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