Reldesemtiv (Synonyms: CK-2127107) |
| カタログ番号GC61239 |
Reldesemtiv (CK-2127107) は、選択的で経口的に活性な次世代速筋トロポニン活性化因子 (FSTA) です。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1345410-31-2
Sample solution is provided at 25 µL, 10mM.
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Reldesemtiv (CK-2127107) is a selective, orally active and next-generation fast skeletal muscle troponin activator (FSTA). Reldesemtiv selectively activates fast skeletal myofibrils with an EC50 of 3.4 μM. Reldesemtiv increases exercise performance in a heart failure model[1].
Reldesemtiv selectively binds to and sensitizes the fast skeletal troponin complex to calcium[1].
Reldesemtiv (10 mg/kg; p.o.) significantly improves rotarod performance in exercise-intolerant LAD-HF rats[1].Reldesemtiv (10 mg/kg; i.v.) increases Ca2+ sensitivity in fast skeletal muscle fibers and increases muscle force in response to submaximal stimulation frequencies in LAD-HF rats[1].Reldesemtiv increases sarcomeric Ca2+ sensitivity in skinned LAD-HF skeletal fibers[1]. Animal Model: Female Sprague-Dawley rats (Sham and left anterior descending coronary artery (LAD) heart failure (LAD-HF))[1]
[1]. Hwee DT, et al. The small-molecule fast skeletal troponin activator, CK-2127107, improves exercise tolerance in a rat model of heart failure. J Pharmacol Exp Ther. 2015 Apr;353(1):159-68. [2]. Andrews JA, et al. CK-2127107 amplifies skeletal muscle response to nerve activation in humans. Muscle Nerve. 2018 May;57(5):729-734.
| Cas No. | 1345410-31-2 | SDF | |
| 同義語 | CK-2127107 | ||
| Canonical SMILES | O=C(C1=CN(C2=CN=C(NC[C@]3(C4=NC=CC=C4F)C[C@H](F)C3)N=C2)C=C1)N | ||
| Formula | C19H18F2N6O | M.Wt | 384.38 |
| 溶解度 | DMSO : 250 mg/mL (650.40 mM; Need ultrasonic) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.6016 mL | 13.008 mL | 26.0159 mL |
| 5 mM | 520.3 μL | 2.6016 mL | 5.2032 mL |
| 10 mM | 260.2 μL | 1.3008 mL | 2.6016 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 7 reference(s) in Google Scholar.)
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