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Tirasemtiv

🥰Excellent
Catalog No. T3966Cas No. 1005491-05-3
Alias CK-2017357

Tirasemtiv (CK-2017357)(CK 2017357) is a small-molecule fast-skeletal-troponin activator, with a potential treatment for muscle weakness and neuromuscular dysfunction.

Tirasemtiv

Tirasemtiv

🥰Excellent
Purity: 98.41%
Catalog No. T3966Alias CK-2017357Cas No. 1005491-05-3
Tirasemtiv (CK-2017357)(CK 2017357) is a small-molecule fast-skeletal-troponin activator, with a potential treatment for muscle weakness and neuromuscular dysfunction.
Pack SizePriceAvailabilityQuantity
5 mg$39In Stock
10 mg$64In Stock
25 mg$143In Stock
50 mg$213In Stock
1 mL x 10 mM (in DMSO)$43In Stock
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Purity:98.41%
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Product Introduction

Bioactivity
Description
Tirasemtiv (CK-2017357)(CK 2017357) is a small-molecule fast-skeletal-troponin activator, with a potential treatment for muscle weakness and neuromuscular dysfunction.
In vitro
Tirasemtiv acts as a fast skeletal troponin activator, enhancing the sarcomere's sensitivity to calcium, thereby magnifying muscle force production in response to diminished neuromuscular input. It specifically increases fast skeletal muscle troponin's responsiveness to calcium (Ca2+), and decelerates the Ca2+ dissociation from the fast skeletal muscle's regulatory troponin complex[1].
In vivo
A single administration of Tirasemtiv significantly enhances muscle strength and endurance—as evidenced by improvements in submaximal isometric force, forelimb grip strength, grid hang time, and rotarod performance—in a female B6SJL-SOD1 g93A transgenic mouse model of ALS exhibiting functional deficits. This treatment also notably increases diaphragm force and tidal volume in these mice. Specifically, Tirasemtiv-treated mice showed a 38% increase in grip strength, rising from 49.6±4.6 g in vehicle-treated mice to 68.6±8.1 g, a statistically significant enhancement (p<0.05, single tailed t-test). The administered dosage regimen of Tirasemtiv was 2 mg/kg at approximately 20-minute intervals, totaling a cumulative dose of 10 mg/kg. Regression analysis further confirmed the efficacy of Tirasemtiv, showing a significant increase in muscle force not only in normal (WT) mice but also in B6SJL-SOD1 g93A mice at mid-stage ALS (WT p<0.0001; mid-stage p=0.0028), with a noted trend towards improved muscle function even at later disease stages (p=0.064)[1].
AliasCK-2017357
Chemical Properties
Molecular Weight230.27
FormulaC12H14N4O
Cas No.1005491-05-3
SmilesCCC(CC)n1c2nc(cnc2[nH]c1=O)C#C
Relative Density.no data available
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 60 mg/mL (260.56 mM)
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM4.3427 mL21.7136 mL43.4273 mL217.1364 mL
5 mM0.8685 mL4.3427 mL8.6855 mL43.4273 mL
10 mM0.4343 mL2.1714 mL4.3427 mL21.7136 mL
20 mM0.2171 mL1.0857 mL2.1714 mL10.8568 mL
50 mM0.0869 mL0.4343 mL0.8685 mL4.3427 mL
100 mM0.0434 mL0.2171 mL0.4343 mL2.1714 mL

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