DGAT-1 inhibitor 2

DGAT-1 inhibitor 2 is an orally active DGAT-1 inhibitor with IC₅₀ values of 15 nM and 9 nM for human DGAT-1 and rat DGAT-1, respectively. DGAT-1 inhibitor 2 increases ROS concentration, GRP78, and PERK protein abundance. DGAT-1 inhibitor 2 increases SREBF1, CPT1A, and MTTP mRNA in fatty acid-treated cells. DGAT-1 inhibitor 2 improves obesity^[1][2]. IC50 & Target:IC₅₀: 15 nM and 9 nM for human DGAT-1 and rat DGAT-1, respectively^[2] In Vitro:DGAT-1 inhibitor 2 (0.3 μM; 12 h) increases the mRNA abundance of SREBF1, CPT1A, and MTTP in fatty acid-treated primary calf hepatocytes^[1].
DGAT-1 inhibitor 2 (Compound 4) shows potent inhibitory activity against DGAT-1, with IC₅₀ values of 15 nM and 9 nM for human DGAT-1 and rat DGAT-1, respectively^[2].
DGAT-1 inhibitor 2 (Compound 4) exhibits excellent potency in inhibiting Triacylglycerol synthesis in human HuTu 80 cells with an IC₅₀ of 3 nM^[2].
In Vivo:DGAT-1 inhibitor 2 (Compound 4) (20 mg/kg; p.o.; once daily; 3 days) causes a modest but statistically significant reduction in body weight (2% compared to start weight, 3% compared to vehicle-treated controls) in diet-induced obesity (DIO) mice fed a high-energy cafeteria diet^[2].
DGAT-1 inhibitor 2 (Compound 4) (0.3 mg/kg; p.o.) significantly reduces plasma triacylglycerol excursion in rats^[2].