Diacylglycerol Acyltransferase Inhibitor-1, a diacylglycerol acyltransferase (DGAT1) inhibitor, effectively suppresses the activity of DGAT1.

OSMI-1 is an O-GlcNAc transferase (OGT) inhibitor (IC50=2.7 μM) that is orally active and cell-permeable. OSMI-1 inhibits protein O-GlcNA acetylation without qualitatively altering cell-surface N- or O- linked glycans.

DGAT-1 inhibitor 2 is an effective DGAT-1 inhibitor; anti-obesity drug. Objective: DGAT-1 acyl-CoA: diacylglycerol acyltransferase 1 (DGAT1) is one of two known DGAT enzymes that catalyze the final step of triglyceride synthesis. The discovery of transgenic mice and pharmacological studies indicate that inhibiting DGAT1 is a promising strategy for treating obesity and type 2 diabetes.

Pradigastat (LCQ-908) is an orally active, potent and selective diacylglycerol acyltransferase 1 (DGAT1) inhibitor for the treatment of constipation, which may be used in the study of obesity and diabetes.

A 922500 (DGAT-1 Inhibitor 4a) is an inhibitor for human and mouse DGAT-1 with IC50 of 7 nM and 24 nM, respectively, good selectivity over related acyltransferases, hERG, and a panel of anti-targets.

PF-07202954, a weakly basic diacylglycerol O-acyltransferase 2 (DGAT2) inhibitor, exhibits an inhibition concentration half-maximum (IC50) of 10 nM against human DGAT2 and effectively reduces liver triglyceride content in a rat model fed on a Western diet [1].

DGAT1-IN-1 is a potent inhibitor of diacylglycerol O- acyltransferase type 1(DGAT1, IC50 of < 10 nM).

T-863(DGAT-1 inhibitor) is an orally active, selective and potent DGAT1 (Acyl-CoA:diacylglycerol acyltransferase 1) inhibitor that interacts with the acyl-CoA binding site of DGAT1, and inhibits triacylglycerol synthesis in cells. IC50 value: Target: DGAT1 T863 (DGAT-3) causes weight loss, reduction in serum and liver triglycerides, and improved insulin sensitivity in obese mice.

1-Methyl-2-[(4Z,7Z)-4,7-tridecadienyl]-4(1H)-quinolone, a diacylglycerol acyltransferase inhibitor and angiotensin II receptor blocker, exhibits IC50 values of 20.1 μM and 34.1 μM, respectively. Additionally, it demonstrates significant anti-Helicobacter pylori activity, boasting a minimum inhibitory concentration (MIC) of 10 μg/mL [1] [2] [3].

AZD3988 is an orally active and highly potent inhibitor of diacylglycerol acyltransferase-1 (DGAT-1) for the study of diabetes and obesity.