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Purity: ≥98%
Tirasemtiv (also known as CK2017357) is a novel small-molecule activator of fast-skeletal-troponin, it is being developed as a potential treatment for diseases and conditions associated with aging, muscle weakness and wasting or neuromuscular dysfunction. Tirasemtiv slows the rate of calcium release from troponin, thus sensitizing fast skeletal muscle fibers to calcium. Tirasemtiv demonstrated increases in skeletal muscle force in response to neuronal input and delays in the onset and reductions in the degree of muscle fatigue.
| ln Vitro |
By sensitizing sarcomeres to calcium, tirasemtiv, a rapid skeletal troponin activator, increases the muscle's responsiveness to neuromuscular input, resulting in increased force production when neural input is decreased. Tirasemtiv reduces the rate of Ca2+ release from fast skeletal muscle-regulated troponin complexes and specifically sensitizes fast skeletal muscle troponin to calcium (Ca2+) [1].
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| ln Vivo |
A single dosage of Tirasemtiv markedly improved submaximal isometric force, forelimb grip strength, grid hang time, and rotational ability in a female transgenic mouse model of ALS with functional impairments (B6SJL-SOD1G93A). Moreover, female B6SJL-SOD1G93A mice treated with Tirasemtiv exhibited considerably increased diaphragm force and tidal volume. Vehicle-treated B6SJL-SOD1G93A mice showed a forelimb grip strength of 49.6 ± 4.6 g at the 25% deficiency milestone. Grip strength rose by 38% with tirasemtiv, reaching 68.6±8.1g (p<0.05, one-tailed t-test). The dosages of tirasemtiv are 2, 2, 2, and 4 mg/kg, spaced about 20 minutes apart, to produce a total dose of 10 mg/kg. Tirasemtiv considerably increased muscle strength in both WT and mid-stage B6SJL-SOD1G93A mice, according to a regression analysis of the log dose-response relationship (WT p<0.0001; mid-stage p=0.0028). Mice that received Tirasemtiv later in the illness demonstrated a tendency toward improved muscular function as compared to baseline (p=0.064) [1].
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| References |
[1]. Hwee DT, et al. Fast skeletal muscle troponin activator tirasemtiv increases muscle function and performance in the B6SJL-SOD1G93A ALS mouse model. PLoS One. 2014 May 7;9(5):e96921
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| Molecular Formula |
C12H14N4O
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|---|---|
| Molecular Weight |
230.26576
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| CAS # |
1005491-05-3
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| Related CAS # |
1005491-05-3;
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| SMILES |
O=C1N(C(CC)CC)C2=NC(C#C)=CN=C2N1
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~10.91 mg/mL (~47.38 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.09 mg/mL (4.73 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 10.9 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 1.09 mg/mL (4.73 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 10.9 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 1.09 mg/mL (4.73 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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