Drug intelligence / Profile preview

EMD-57033

Development stage
Preclinical
Lead developer
Merck
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

EMD-57033 is a small molecule positive inotropic agent and calcium sensitizer originally developed by Merck KGaA. It belongs to the thiadiazinone chemical class and acts as a cardiac myosin activator. Unlike traditional inotropes that increase intracellular calcium levels, EMD-57033 enhances the sensitivity of the cardiac myofilaments to calcium and stabilizes the force-producing state of myosin heads. Specifically, it has been shown to recruit myosin heads from the super-relaxed (SRX) state into active, force-generating states. While it was historically investigated for the treatment of heart failure, it is currently used primarily as a pharmacological research tool to study cardiac muscle mechanics and the regulation of the thick filament.

Other names
(+)-EMD 57033
02

Targets

TNNC1 (Cardiac troponin C)MYH7 (Cardiac beta-myosin heavy chain)

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