CK-2017357 MedChemExpress (MCE)

Product Name	Tirasemtiv
Synonyms	CK 2017357 TiraseMtiv Tirasemtiv TIRASEMTIV(CK-2017357) Tirasemtiv(CK-2017357) tiraseMtiv (CK-2017357) 6-ethynyl-1-(pentan-3-yl)-1H-iMidazo[4,5-b]pyrazin-2-ol Synonyms CK 2017357 TiraseMtiv Tirasemtiv TIRASEMTIV(CK-2017357) Tirasemtiv(CK-2017357) tiraseMtiv (CK-2017357) 6-ethynyl-1-(pentan-3-yl)-1H-iMidazo[4,5-b]pyrazin-2-ol 6-ETHYNYL-1-(PENTAN-3-YL)-1H-IMIDAZO[4,5-B]PYRAZIN-2(3H)-ONE 1-(1-Ethylpropyl)-6-ethynyl-1,3-dihydro-2H-imidazo[4,5-b]pyrazin-2-one Tirasemtiv 1-(1-Ethylpropyl)-6-ethynyl-1,3-dihydro-2H-imidazo[4,5-b]pyrazin-2-one Tirasemtiv 1-(1-Ethylpropyl)-6-ethynyl-1,3-dihydro-2H-imidazo[4,5-b]pyrazin-2-one
CAS	1005491-05-3
EINECS
Chemical Formula	C12H14N4O
Molecular Weight	230.27
inchi
Package	10 mM * 1 mL;5 mg;10 mg;25 mg;50 mg;100 mg
Price	Email to quote
Descriptions	Tirasemtiv Tirasemtiv MedChemExpress (MCE) HY-15964 1005491-05-3 CK-2017357 99.90% Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year Room temperature in continental US Descriptions Tirasemtiv Tirasemtiv MedChemExpress (MCE) HY-15964 1005491-05-3 CK-2017357 99.90% Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year Room temperature in continental US may vary elsewhere. Tirasemtiv is an activator of the fast skeletal muscle troponin complex. Tirasemtiv is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups. 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]. 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 (pG93A mice (WT p[1]. Mice[1] Wild-type background strain B6SJLF1/J mice and B6SJL-SOD1G93A mice over-expressing the human SOD-1 gene with mutation G93A are group-housed in a 12-hour light cycle and fed standard chow and water ad libitum. Tirasemtiv is administered in solution (50% PEG300/10% EtOH/40% Cavitron cyclodextrin formulation) as a single slow bolus over a 2 minute period via a catheter in the contralateral femoral artery placed above the aortic bifurcation. Tirasemtiv bolus injections (2, 2, 2, and 4 mg/kg) are given at approximately 20 min intervals to achieve a cumulative dose of 10 mg/kg in order to assess the dose response, with a maximal dosage volume of 5 mL/kg. At the end of each experiment, a single terminal blood sample is drawn via cardiac puncture for compound concentration analysis. Troponin[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]. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> Tirasemtiv Related Antibodies \| \| \| \| \| \| \| \| \| \| [1]. Hwee DT, 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. [Content Brief]
Last Update	2025-04-01 14:45:47

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