A cardiac myosin ATPase inhibitor (IC50 = 0.3 µM); selective for cardiac myosin over skeletal myosin (IC50 = 4.7 µM); slows ATPase activity of α- and β-myosin; reduces cardiac contractility

MYK-461 – 5 mg

Brand:
Cayman
CAS:
1642288-47-8
Storage:
-20
UN-No:
Non-Hazardous - /

MYK-461 is an orally bioavailable inhibitor of cardiac myosin ATPase (IC50 = 0.3 µM in purified bovine myosin S1).{30587} It is selective for cardiac myosin over skeletal myosin (IC50 = 4.7 µM) and does not induce skeletal muscle impairments. It slows the rate of ATPase activity in both murine and bovine myofibrils, which are α- and β-myosin-rich, respectively, by reducing the rate of phosphate release during the myosin power stroke. In transgenic mouse models of hypertrophic cardiomyopathy, MYK-461 reduces cardiac contractility, prevents left ventricular hypertrophy, and reverses pathologic remodeling. In cats, it relieves left ventricular outflow tract obstruction.{40089} Formulations containing MYK-461 have been used for the treatment of symptomatic hypertrophic cardiomyopathy in humans and cats.  

 

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Description

A cardiac myosin ATPase inhibitor (IC50 = 0.3 µM); selective for cardiac myosin over skeletal myosin (IC50 = 4.7 µM); slows ATPase activity of α- and β-myosin; reduces cardiac contractility, prevents left ventricular hypertrophy, and reverses pathologic remodeling in mouse models; relieves left ventricular outflow tract obstruction in cats

Formal name: 3-(1-methylethyl)-6-[[(1S)-1-phenylethyl]amino]-2,4(1H,3H)-pyrimidinedione

Synonyms:  SAR439152

Molecular weight: 273.3

CAS: 1642288-47-8

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|ATPases||Product Type|Biochemicals|Transporter & Exchanger Modulators||Research Area|Cardiovascular System|Cardiovascular Diseases|Cardiomyopathy||Research Area|Cardiovascular System|Heart|Myocardial Contractility||Research Area|Cardiovascular System|Heart|Myocardial Hypertrophy

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