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CAS No.: 701232-20-4

T863 Catalog No. CSN12799

Synonyms: DGAT-1 Inhibitor;DGAT-3

T863 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.

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400-920-2911

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技术信息

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].
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

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.5351 mL
- 12.6753 mL
- 25.3507 mL
- 5 mM
- 0.5070 mL
- 2.5351 mL
- 5.0701 mL
- 10 mM
- 0.2535 mL
- 1.2675 mL
- 2.5351 mL

技术信息

CAS号

701232-20-4

储存条件

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

液体: -20°C:3-6 月 -80°C:12月

分子式

C22H26N4O3

运输

蓝冰

分子量

394.47

别名

DGAT-1 Inhibitor;DGAT-3

溶解度

DMSO	79.0 mg/mL (200.3 mM)
Water	Insoluble
Ethanol	1.0 mg/mL (2.5 mM)

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