Drug intelligence / Profile preview

CI-976

Development stage
Preclinical
Lead developer
Pfizer
Modality
Small Molecules
Administration
Oral
01

Overview

CI-976 is a potent, orally active, and selective small molecule inhibitor of acyl-coenzyme A:cholesterol acyltransferase (ACAT, also known as sterol O-acyltransferase or SOAT), with an IC50 of approximately 73 nM. It blocks cholesterol esterification by inhibiting both ACAT1 and ACAT2 isozymes, and also inhibits lysophospholipid acyltransferase (LPAT) activity at higher concentrations. CI-976 lowers non-HDL cholesterol and increases HDL in animal models of dyslipidemia. Structurally, it is an anilide and lysophospholipid acyltransferase antagonist from the fatty acyl amide analog family. It is used primarily as a tool compound in research settings, not for therapeutic use, and has been widely cited in studies of cholesterol metabolism, lipid droplet biology, and membrane trafficking[1][2][4][5][7][8][9][13][14][15].

Other names
2,2-dimethyl-N-(2,4,6-trimethoxyphenyl)dodecanamide
02

Targets

ACAT1 (Acyl-coenzyme A:cholesterol O-acyltransferase 1)AGPAT3 (1-acyl-sn-glycerol-3-phosphate acyltransferase 3)NMBR (Neuromedin B receptor)

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