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Tirasemtiv (Synonyms: CK-2017357)

Cat. No.: HY-15964 Purity: 99.47%
Handling Instructions

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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Based on 1 publication(s) in Google Scholar

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Description

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

IC50 & Target

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].

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

230.27

Formula

C₁₂H₁₄N₄O

CAS No.

1005491-05-3

SMILES

O=C1N(C(CC)CC)C2=NC(C#C)=CN=C2N1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
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.

Preparing
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.
References
Animal Administration
[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.

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

References
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Keywords:

TirasemtivCK-2017357CK2017357CK 2017357OthersInhibitorinhibitorinhibit

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