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T863

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Chemical Structure| 701232-20-4 同义名 : DGAT-3
CAS号 : 701232-20-4
货号 : A318437
分子式 : C22H26N4O3
纯度 : 99%+
分子量 : 394.467
MDL号 : MFCD11977270
存储条件：

粉末 Keep in dark place,Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(126.75 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 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 circulation[3].
作用机制 T863 binds to the oleoyl-CoA binding site of DGAT1 bound with 1,2-DOG[3].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.54mL

0.51mL

0.25mL

12.68mL

2.54mL

1.27mL

25.35mL

5.07mL

2.54mL
参考文献

[1]Cao J, Zhou Y, et al. Targeting Acyl-CoA:diacylglycerol acyltransferase 1 (DGAT1) with small molecule inhibitors for the treatment of metabolic diseases. J Biol Chem. 2011 Dec 2;286(48):41838-51.

[2]Dow RL, Andrews M, et al. Design and synthesis of potent, orally-active DGAT-1 inhibitors containing a dioxino[2,3-d] pyrimidine core. Bioorg Med Chem Lett. 2011 Oct 15;21(20):6122-5.

[3]Cao J, Zhou Y, Peng H, Huang X, Stahler S, Suri V, Qadri A, et al. Targeting Acyl-CoA:diacylglycerol acyltransferase 1 (DGAT1) with small molecule inhibitors for the treatment of metabolic diseases. J Biol Chem. 2011 Dec 2;286(48):41838-51