T863

Acyl-CoA:diacylglycerol acyltransferase 1 (DGAT1) is one of two known DGAT enzymes that catalyze the final step in triglyceride synthesis. Inhibition of DGAT1 is a promising strategy for the treatment of obesity and type 2 diabetes. T863 is a potent and specific DGAT1 inhibitor with respect to oleoyl-CoA with IC₅₀ values of 49 nM and 17 nM in the CPM fluorescent assay and the TLC assay, respectively. T863 showed a dose-dependent inhibition of the binding of radiolabeled oleoyl-CoA to DGAT1. T863 caused a dose-dependent inhibition of cellular triacylglycerol (TAG) formation in HEK293-DGAT1 cells with an IC₅₀ of 122 nM. In an acute lipid challenge model using C57/BL6 mice, administration of the corn oil bolus resulted in a significant, 60% increase in serum triglyceride levels in vehicle-treated animals, while no increase was observed in mice treated with 10 mg/kg T863 indicating T863 inhibits acute lipid absorption. Administration of T863 (30 mg/kg for 15 days) to DIO (diet-induced obese) mice caused a reduction in body weight, which reached statistical significance by the 13th day of treatment. Moreover, T863-treated DIO mice showed a modest improvement in clearing glucose from peripheral circulation³.

溶解方案(细胞实验)

DMSO 中的溶解度 : ≥ 50 mg/mL (126.75 mM; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)|* "≥" means soluble, but saturation unknown.

溶解方案(动物实验)

"方案 一": "请依序添加每种溶剂：10% DMSO 90% Corn OilSolubility: ≥ 2.5 mg/mL (6.34 mM); 澄清溶液 此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。"