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Reldesemtiv (Synonyms: CK-2127107)

Cat. No.: HY-109121
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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.

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Reldesemtiv Chemical Structure

Reldesemtiv Chemical Structure

CAS No. : 1345410-31-2

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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[1].

In Vitro

Reldesemtiv selectively binds to and sensitizes the fast skeletal troponin complex to calcium[1].

In Vivo

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]
Dosage: 10 mg/kg
Administration: p.o.
Result: Increased performance time by approximately 150% in LAD-HF rats (116±22 versus 283±47 seconds).
Molecular Weight

384.38

Formula

C₁₉H₁₈F₂N₆O

CAS No.

1345410-31-2

SMILES

O=C(C1=CN(C2=CN=C(NC[[email protected]]3(C4=NC=CC=C4F)C[[email protected]](F)C3)N=C2)C=C1)N

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Keywords:

ReldesemtivCK-2127107CK2127107CK 2127107Othersnext-generationskeletalmyofibrilsexerciseperformancecalciumheartfailureInhibitorinhibitorinhibit

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