A cardiac-specific myosin activator
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Danicamtiv

Item No. 36875

Technical Information
Formal Name
4-[(1R)-1-[[3-(difluoromethyl)-1-methyl-1H-pyrazol-4-yl]sulfonyl]-1-fluoroethyl]-N-3-isoxazolyl-1-piperidinecarboxamide
CAS Number
1970972-74-7
Synonyms
  • MYK-491
  • SAR440181
Molecular Formula
C16H20F3N5O4S
Formula Weight
Purity
≥98%
Formulation
A solid
DMF: 5 mg/mlDMSO: 5 mg/ml
SMILES
C[C@](F)(C1CCN(CC1)C(NC2=NOC=C2)=O)S(=O)(C3=CN(C)N=C3C(F)F)=O
InChi Code
InChI=1S/C16H20F3N5O4S/c1-16(19,29(26,27)11-9-23(2)21-13(11)14(17)18)10-3-6-24(7-4-10)15(25)20-12-5-8-28-22-12/h5,8-10,14H,3-4,6-7H2,1-2H3,(H,20,22,25)/t16-/m1/s1
InChi Key
NREKKBAMVWQRES-MRXNPFEDSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    Danicamtiv is a cardiac-specific myosin activator.1,2 It activates human cardiac S1 myosin when used at a concentration of 3 µM but does not activate skeletal or smooth muscle myosin.1 It increases sarcomere activity of isolated porcine left ventricular and atrial myofibrils with 50% active concentration values (AC50s) of 6 and 3.6 µM, respectively. Danicamtiv (3 µM) increases calcium sensitivity of isolated porcine skinned left ventricular and atrial fibers. Danicamtiv (2-3 mg/kg) also prolongs systolic ejection time and improves left ventricular ejection fraction and stroke volume in a dog model of heart failure.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Voors, A.A., Tamby, J.-F., Cleland, J.G., et alEffects of danicamtiv, a novel cardiac myosin activator, in heart failure with reduced ejection fraction: experimental data and clinical results from a phase 2a trial. Eur. J. Heart Fail. 22(9), 1649-1658 (2020).

    2. Grillo, M.P., Markova, S., Evanchik, M., et alPreclinical in vitro and in vivo pharmacokinetic properties of danicamtiv, a new targeted myosin activator for the treatment of dilated cardiomyopathy. Xenobiotica 51(2), 222-238 (2021).