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Tirasemtiv (Synonyms: CK-2017357)

Cat. No.: HY-15964 Purity: 99.47%
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Tirasemtiv is an activator of the fast skeletal muscle troponin complex.

For research use only. We do not sell to patients.

Tirasemtiv Chemical Structure

Tirasemtiv Chemical Structure

CAS No. : 1005491-05-3

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10 mM * 1 mL in DMSO USD 132 In-stock
Estimated Time of Arrival: December 31
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10 mg USD 168 In-stock
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Based on 1 publication(s) in Google Scholar

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Tirasemtiv is an activator of the fast skeletal muscle troponin complex.

IC50 & Target


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].

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].

Clinical Trial
Molecular Weight









Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 52 mg/mL (225.82 mM)

*"≥" means soluble, but saturation unknown.

Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 4.3427 mL 21.7136 mL 43.4273 mL
5 mM 0.8685 mL 4.3427 mL 8.6855 mL
10 mM 0.4343 mL 2.1714 mL 4.3427 mL
*Please refer to the solubility information to select the appropriate solvent.
Animal Administration

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.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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TirasemtivCK-2017357CK2017357CK 2017357OthersInhibitorinhibitorinhibit

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