| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| Other Sizes |
|
Reldesemtiv (CK2127107; CK-2127107; CK107; CK-107) is a novel, potent and second-generation fast skeletal muscle troponin activator (FSTA) with the potential for the Treatment of Impaired Muscle Function. It increases force production at submaximal stimulation frequencies. Reldesemtiv demonstrated increased muscle force generation in a phase 1 clinical trial and is currently being evaluated in clinical trials for the treatment of amyotrophic lateral sclerosis.
| ln Vitro |
Reldesemtiv causes calcium sensitivity by binding to the fast dual troponin complex [1].
|
|---|---|
| ln Vivo |
Exercise-intolerant LAD-HF stent users' rotary rod performance is markedly enhanced by reldesemtiv (10 mg/kg; neck) [1]. The Ca 2+ architecture of fast junction muscle fibers in LAD-HF scaffolds is increased by reldesemtiv (10 mg/kg; iv), and this results in an increase in force that corresponds to submaximal stimulation frequency [1]. Sarcomeric Ca2+ body weight of cutaneous LAD-HF connected fibers is increased by reldesemtiv [1].
|
| Animal Protocol |
Animal/Disease Models: Female SD (SD (Sprague-Dawley)) rats (Sham and Sham ). Left anterior descending coronary artery (LAD) heart failure (LAD-HF))[1]
Doses: 10 mg/kg Route of Administration: Oral Experimental Results: LAD-HF rats demonstrated approximately 150% increase in performance time (116±22 vs. 283 ±47) seconds). |
| References |
[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. |
| Additional Infomation |
Reldesemtiv is under investigation in clinical trial NCT03160898 (A Study to Evaluate Efficacy, Safety and Tolerability of CK-2127107 in Patients With Amyotrophic Lateral Sclerosis (ALS)).
Drug Indication Treatment of amyotrophic lateral sclerosis |
| Molecular Formula |
C19H18F2N6O
|
|---|---|
| Molecular Weight |
384.39
|
| Exact Mass |
384.151
|
| CAS # |
1345410-31-2
|
| Related CAS # |
Reldesemtiv HCl;
|
| PubChem CID |
67454400
|
| Appearance |
White to off-white solid powder
|
| Density |
1.5±0.1 g/cm3
|
| Boiling Point |
642.4±65.0 °C at 760 mmHg
|
| Flash Point |
342.3±34.3 °C
|
| Vapour Pressure |
0.0±1.9 mmHg at 25°C
|
| Index of Refraction |
1.691
|
| LogP |
0.71
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
7
|
| Rotatable Bond Count |
6
|
| Heavy Atom Count |
28
|
| Complexity |
553
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
FC1CC(C2C(=CC=CN=2)F)(CNC2N=CC(=CN=2)N2C=CC(C(N)=O)=C2)C1
|
| InChi Key |
MQXWPWOCXGARRK-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C19H18F2N6O/c20-13-6-19(7-13,16-15(21)2-1-4-23-16)11-26-18-24-8-14(9-25-18)27-5-3-12(10-27)17(22)28/h1-5,8-10,13H,6-7,11H2,(H2,22,28)(H,24,25,26)
|
| Chemical Name |
1-[2-[[3-fluoro-1-(3-fluoropyridin-2-yl)cyclobutyl]methylamino]pyrimidin-5-yl]pyrrole-3-carboxamide
|
| Synonyms |
CK2127107 CK-107 CK 2127107CK 107 CK107 Reldesemtiv, CK-2127107
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
DMSO : ~250 mg/mL (~650.40 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.41 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 20.8 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: ≥ 2.08 mg/mL (5.41 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 20.8 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: ≥ 2.08 mg/mL (5.41 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 | 2.6015 mL | 13.0076 mL | 26.0152 mL | |
| 5 mM | 0.5203 mL | 2.6015 mL | 5.2030 mL | |
| 10 mM | 0.2602 mL | 1.3008 mL | 2.6015 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
