Tirasemtiv

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Tirasemtiv

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Cat No: 26075

Biochemicals - Small Molecule Activators

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 ...

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Territorial Availability: Available through Bertin Technologies only in France

Synonyms:

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

Correlated keywords:

1360624-92-5 1360874-10-7 CK2017357

Product Overview:
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}

Size	5 mg
Shipping	dry ice
CAS Number	1005491-05-3
Molecular Formula	C₁₂H₁₄N₄O
SMILES	O=C1N(C(CC)CC)C2=NC(C#C)=CN=C2N1
Molecular Weight	230,3
Formulation	A crystalline solid
Purity	≥98%
Custom Code	2921.30
UNSPSC code	12352100

Technical File

MSDS

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Cayman Chemical's mission is to help make research possible by supplying scientists worldwide with the basic research tools necessary for advancing human and animal health. Our utmost commitment to healthcare researchers is to offer the highest quality products with an affordable pricing policy.

Our scientists are experts in the synthesis, purification, and characterization of biochemicals ranging from small drug-like heterocycles to complex biolipids, fatty acids, and many others. We are also highly skilled in all aspects of assay and antibody development, protein expression, crystallization, and structure determination.

Over the past thirty years, Cayman developed a deep knowledge base in lipid biochemistry, including research involving the arachidonic acid cascade, inositol phosphates, and cannabinoids. This knowledge enabled the production of reagents of exceptional quality for cancer, oxidative injury, epigenetics, neuroscience, inflammation, metabolism, and many additional lines of research.

Our organic and analytical chemists specialize in the rapid development of manufacturing processes and analytical methods to carry out clinical and commercial GMP-API production. Pre-clinical drug discovery efforts are currently underway in the areas of bone restoration and repair, muscular dystrophy, oncology, and inflammation. A separate group of Ph.D.-level scientists are dedicated to offering Hit-to-Lead Discovery and Profiling Services for epigenetic targets. Our knowledgeable chemists can be contracted to perform complete sample analysis for analytes measured by the majority of our assays. We also offer a wide range of analytical services using LC-MS/MS, HPLC, GC, and many other techniques.

Accreditations
ISO/IEC 17025:2005
ISO Guide 34:2009

Cayman is a leader in the field of emerging drugs of abuse, providing high-purity Schedule I-V Controlled Substances to federally-licensed laboratories and qualified academic research institutions for forensic analyses. We are certified by ACLASS Accreditation Services with dual accreditation to ISO/IEC 17025:2005 and ISO Guide 34:2009.