An activator of the fast skeletal troponin complex; selectively binds to purified fast skeletal troponin complex (Kd = 40 nM) over slow skeletal (Kd = 3

Tirasemtiv – 10 mg

Brand:
Cayman
CAS:
1005491-05-3
Storage:
-20
UN-No:
Non-Hazardous - /

Tirasemtiv is an activator of the fast skeletal troponin complex.{36966} It selectively binds to purified fast skeletal troponin complex (Kd = 40 nM) over slow skeletal (Kd = 3,800 nM) and cardiac troponin complexes. Tirasemtiv (20 μM) slows the rate of calcium release from the fast skeletal troponin complex. It increases the ATPase activity of isolated rabbit fast skeletal myofibrils at a fixed calcium concentration (EC50 = 390 nM) and sensitizes skinned fast skeletal muscle fibers isolated from human and rabbit to calcium in a concentration-dependent manner. Tirasemtiv increases in situ extensor digitorum longus (EDL) muscle force and forelimb grip strength in a rat model of myasthenia gravis. It also increases forelimb grip strength, grid hang test performance, and rotarod performance in a mouse model of amyotrophic lateral sclerosis (ALS) when administered at a dose of 10 mg/kg.{36967}  

 

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Description

An activator of the fast skeletal troponin complex; selectively binds to purified fast skeletal troponin complex (Kd = 40 nM) over slow skeletal (Kd = 3,800 nM) and cardiac troponin complexes; slows the rate of calcium release from the fast skeletal troponin complex at 20 μM; increases the ATPase activity of isolated rabbit fast skeletal myofibrils at a fixed calcium concentration (EC50 = 390 nM); sensitizes skinned fast skeletal muscle fibers isolated from human and rabbit to calcium; increases in situ EDL muscle force and forelimb grip strength in a rat model of myasthenia gravis; increases forelimb grip strength, grid hang test performance, and rotarod performance in a mouse model of ALS at 10 mg/kg

Formal name: 1-(1-ethylpropyl)-6-ethynyl-1,3-dihydro-2H-imidazo[4,5-b]pyrazin-2-one

Synonyms:  CK-2017357

Molecular weight: 230.3

CAS: 1005491-05-3

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Activators||Research Area|Neuroscience|Neurodegenerative Disorders

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