An activator of fast skeletal troponin
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Reldesemtiv

Item No. 41840

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
1-[2-[[[trans-3-fluoro-1-(3-fluoro-2-pyridinyl)cyclobutyl]methyl]amino]-5-pyrimidinyl]-1H-pyrrole-3-carboxamide
CAS Number
1345410-31-2
Synonyms
  • CK-2127107
Molecular Formula
C19H18F2N6O
Formula Weight
384.4
Purity
≥95%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Sparingly soluble: 1-10 mg/ml
SMILES
FC(C=CC=N1)=C1[C@]2(C[C@H](F)C2)CNC(N=C3)=NC=C3N4C=C(C(N)=O)C=C4
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)/t13-,19-
InChi Key
MQXWPWOCXGARRK-HJGJAMNPSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $102

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    5 mg

    $405

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    10 mg

    $608

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    25 mg

    $1,012

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    Product Description

    Reldesemtiv is an activator of fast skeletal troponin.1 It increases ATPase activity in isolated rabbit psoas muscle myofibril preparations with a 40% activation concentration (AC40) value of 0.6 µM. Reldesemtiv is selective for fast skeletal troponin over cardiac and slow skeletal troponin.2 It is also selective for fast skeletal troponin over a panel of 79 enzymes, receptors, ion channels, and transporters at 100 µM.1 Reldesemtiv increases muscle tension in a skinned fast skeletal muscle fiber assay with a 30% muscle force (DF30) value of 0.8 µM.1 In vivo, reldesemtiv (10 mg/kg, p.o.) increases running time in the rotarod test, indicating increased exercise performance, in a rat model of heart failure-induced skeletal myopathy.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Collibee, S.E., Bergnes, G., Chuang, C., et al. Discovery of Reldesemtiv, a Fast Skeletal Muscle Troponin Activator for the Treatment of Impaired Muscle Function. J. Med. Chem. 64(2), 14930-14941 (2021).

    2. Hwee, D.T., Kennedy, A.R., Hartman, J.J., 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. 353(1), 159-168 (2015).