Description
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.
Product information
CAS Number: 1345410-31-2
Molecular Weight: 384.38
Formula: C19H18F2N6O
Chemical Name: 1-[2-({[3-fluoro-1-(3-fluoropyridin-2-yl)cyclobutyl]methyl}amino)pyrimidin-5-yl]-1H-pyrrole-3-carboxamide
Smiles: NC(=O)C1=CN(C=C1)C1=CN=C(NCC2(CC(F)C2)C2=NC=CC=C2F)N=C1
InChiKey: MQXWPWOCXGARRK-UHFFFAOYSA-N
InChi: 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)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 250 mg/mL (650.40 mM; Need ultrasonic).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
Reldesemtiv selectively binds to and sensitizes the fast skeletal troponin complex to calcium.
In Vivo:
Reldesemtiv (10 mg/kg; p.o.) significantly improves rotarod performance in exercise-intolerant LAD-HF rats. 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. Reldesemtiv increases sarcomeric Ca2+ sensitivity in skinned LAD-HF skeletal fibers.
Products are for research use only. Not for human use.
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