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MYK-461
- Mavacamten - SAR439152
- Optical Purity: Optically pure
- Soluble in 0.1N NaOH(aq) and DMSO
- MF: C15H19N3O2
- MW: 273.33
Description
MYK-461 (Mavacamten, SAR439152) , also known as mavacamten, is a selective allosteric inhibitor of cardiac myosin that decreases sarcomere contractility by reducing myosin ATPase activity. It inhibits ATPase activity in mouse cardiac myofibrils with an IC50 of approximately 0.3 µM, reducing the number of force-generating actin–myosin cross-bridges without directly blocking calcium handling.
MYK-461 is a critical translational tool linking myosin enzymology to contractile disease phenotypes by mitigating sarcomeric hypercontractility, preventing hypertrophy, and relieving acute outflow obstruction in preclinical cardiomyopathy models.
Key Features
- Selective allosteric inhibitor of cardiac myosin
- IC50: approximately 0.3 µM in mouse cardiac myofibrils
- Reduces myosin ATPase activity and sarcomere contractility
- Decreases force-generating actin–myosin cross-bridges
- Validated in hypertrophic cardiomyopathy models
Applications
- Cardiac myosin pharmacology
- Sarcomere contraction and cross-bridge cycling
- Hypertrophic cardiomyopathy research
- Left ventricular outflow tract obstruction models
- Cardiac contractility assays
More Information
| Parent CAS No. | 1642288-47-8 |
|---|---|
| Chemical Name | (S)-3-Isopropyl-6-(1-phenylethylamino)pyrimidine-2,4(1H,3H)-dione |
| SMILES | C1C=C([C@H](C)NC2=CC(=O)N(C(C)C)C(=O)N2)C=CC=1 |&1:3,r| |
| MFCD | N.A. |
| InChi | InChI=1S/C15H19N3O2/c1-10(2)18-14(19)9-13(17-15(18)20)16-11(3)12-7-5-4-6-8-12/h4-11,16H,1-3H3,(H,17,20)/t11-/m0/s1 |
| InChiKey | RLCLASQCAPXVLM-NSHDSACASA-N |
| CID | 117761397 |
| Short Description | Myosin inhibitor |
References
- EM Green et al. A small-molecule inhibitor of sarcomere contractility suppresses hypertrophic cardiomyopathy in mice. Science. 2016 Feb 5;351(6273):617-21.
- JA Stern et al. A Small Molecule Inhibitor of Sarcomere Contractility Acutely Relieves Left Ventricular Outflow Tract Obstruction in Feline Hypertrophic Cardiomyopathy. PLoS One. 2016 Dec 14;11(12):e0168407.
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