T863

T863 is a potent, small-molecule inhibitor of diacylglycerol O-acyltransferase 1 (DGAT1), an integral membrane protein that catalyzes the final and rate-limiting step in the synthesis of triacylglycerols (TG). Developed as a tool compound, T863 functions by binding to the acyl-CoA substrate binding tunnel of DGAT1, effectively blocking the entrance and preventing the conversion of diacylglycerol and fatty acyl-CoA into triglycerides. Preclinical research has demonstrated that T863 can reduce body weight, lower serum and liver triglyceride levels, and improve insulin sensitivity in models of obesity and type 2 diabetes. Beyond metabolic disorders, T863 has shown promise in treating infectious diseases such as Tuberculosis and Toxoplasmosis by modulating host or pathogen lipid metabolism, and it is being investigated in oncology as a component of pH-responsive drug delivery systems to target the acidic microenvironment of tumors.