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Tirasemtiv

  Cat. No.:  DC7518   Featured
Chemical Structure
1005491-05-3
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More than 5000 active chemicals with high quality for research!
Field of application
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.
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 1005491-05-3
Chemical Name: CK-2017357; CK2017357; CK 2017357
Synonyms: CK-2017357; CK2017357; CK 2017357
SMILES: C12N(C(CC)CC)C(=O)NC1=NC=C(C#C)N=2
Formula: C12H14N4O
M.Wt: 230.27
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: Tirasemtiv is an activator of the fast skeletal muscle troponin complex.
In Vivo: A single dose of Tirasemtiv significantly increases submaximal isometric force, forelimb grip strength, grid hang time, and rotarod performance in a female transgenic mouse model (B6SJL-SOD1G93A) of ALS with functional deficits. Additionally, diaphragm force and tidal volume are significantly higher in Tirasemtiv-treated female B6SJL-SOD1G93A mice. At the 25% deficit milestone, vehicle-treated B6SJL-SOD1G93A mice demonstrated forelimb grip strength of 49.6±4.6 g. Tirasemtiv increases grip strength by 38% to 68.6±8.1g (p<0.05, single tailed t-test). Tirasemtiv doses of 2, 2, 2, and 4 mg/kg given at approximately 20 min intervals to achieve a cumulative dose of 10 mg/kg. Regression analysis of the log dose vs. response relationship indicated that Tirasemtiv significantly increased muscle force in WT and mid-stage B6SJL-SOD1G93A mice (WT p<0.0001; mid-stage p=0.0028). At later stages of disease, the mice exhibited a trend for increased muscle function in response to Tirasemtivcompared to baseline (p=0.064)[1].
In Vitro: Tirasemtiv is a fast skeletal troponin activator that sensitizes the sarcomere to calcium; this mechanism of action amplifies the response of muscle to neuromuscular input producing greater force when nerve input is reduced. Tirasemtiv selectively sensitizes fast skeletal muscle troponin to calcium (Ca2+), and slows the rate of Ca2+ release from the regulatory troponin complex of fast skeletal muscle[1].
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
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