CGP-37157

CGP-37157 is a small molecule benzothiazepine derivative originally developed by Novartis for the treatment of cardiovascular diseases. It is primarily characterized as a selective inhibitor of the mitochondrial Na+/Ca2+ exchanger (NCLX), which regulates the efflux of calcium from the mitochondria into the cytosol. By inhibiting NCLX, CGP-37157 modulates mitochondrial calcium dynamics, which has significant implications for cellular metabolism and signaling. In addition to its primary target, the compound has been found to inhibit the sarcoplasmic reticulum Ca2+ ATPase (SERCA), activate ryanodine receptor (RyR) channels, and block Calcium Homeostasis Modulator 1 (CALHM1) channels. Although its clinical development for cardiovascular indications was discontinued, it remains a widely utilized pharmacological tool in research for studying intracellular calcium homeostasis and has recently been investigated in preclinical models of epilepsy and status epilepticus.

Other names

7-Chloro-5-(2-chlorophenyl)-1,5-dihydro-4,1-benzothiazepin-2(3H)-one7-chloro-5-(2-chlorophenyl)-3,5-dihydro-4,1-benzothiazepin-2-(1H)-one