VB-85387 is a potent and selective inhibitor of monoacylglycerol acyltransferase 2 (MOGAT2, MGAT2) with IC50 of 11.0 nM and 10.4 nM against human and mouse MGAT2 respectively.
VB-85387 displays >1000-fold selectivity over related acyltransferases, including MOGAT1/3, DGAT1/2, ACAT1/2, and AWAT1/2.
VB-85387 (30 mg/kg) shows reduced the development of MASLD and fibrosis in the LMCD model.
VB-85387 restores normal triglyceride levels in mice fed the LMCD diet.
VB-85387 restores intestinal and fecal lipid homeostasis in LMCD-fed female mice.
VB-85387 reduces MASLD and fibrosis in LMCD-fed mice.
VB-85387 reduces type I and III collagen protein levels in mice fed the LMCD diet.
VB-85387 induces PPARα signaling while reducing SREBP1-dependent transcription (SREBF1, ACC1, and FASN) in high-fat diet-induced obese mice.
VB-85387 reduces adipocyte cell size and restores adipocyte cell number in LMCD-fed mice.