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Reldesemtiv (Synonyms: CK-2127107)

Cat. No.: HY-109121 Purity: 99.51%
Handling Instructions

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.

For research use only. We do not sell to patients.

Reldesemtiv Chemical Structure

Reldesemtiv Chemical Structure

CAS No. : 1345410-31-2

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 528 In-stock
Estimated Time of Arrival: December 31
5 mg USD 480 In-stock
Estimated Time of Arrival: December 31
10 mg USD 800 In-stock
Estimated Time of Arrival: December 31
25 mg USD 1550 In-stock
Estimated Time of Arrival: December 31
50 mg USD 2500 In-stock
Estimated Time of Arrival: December 31
100 mg USD 3800 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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).
Clinical Trial
Molecular Weight

384.38

Formula

C₁₉H₁₈F₂N₆O

CAS No.
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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (650.40 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6016 mL 13.0080 mL 26.0159 mL
5 mM 0.5203 mL 2.6016 mL 5.2032 mL
10 mM 0.2602 mL 1.3008 mL 2.6016 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (5.41 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (5.41 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (5.41 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

ReldesemtivCK-2127107CK2127107CK 2127107Othersnext-generationskeletalmyofibrilsexerciseperformancecalciumheartfailureInhibitorinhibitorinhibit

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Reldesemtiv
Cat. No.:
HY-109121
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