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编 号:F430766
分子式:C22H26N4O3
分子量:394.47
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10mM*1mL in DMSO
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1mg
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5mg
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10mg
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25mg
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50mg
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生物活性:
T863 is an orally active, selective and potent DGAT1 (acyl-CoA:diacylglycerol acyltransferase 1) inhibitor with an IC50 of 15 nM. T863 has no inhibitory activity against human MGAT3, human DGAT2, or human MGAT2. T863 interacts with the acyl-CoA binding site of DGAT1, and inhibits triacylglycerol synthesis in cells.

体内研究:
T863(30 mg/kg;口服)可导致体重减轻、血清和肝脏甘油三酯降低,并改善胰岛素敏感性。Animal Model:C57BL6 normal mice (8 weeks old) or diet-induced obese (DIO) mice (10 months old, fed a high fat diet for 8 months)
Dosage:30 mg/kg (5 μL/g)
Administration:Oral administration; once a day for days 1-7 and twice a day for days 8-14
Result:Significantly delayed fat absorption and resulted in lipid accumulation in the distal small intestine of mice, mimicking the effects of genetic ablation of DGAT1.

体外研究:
T863(持续 3 天)增强胰岛素刺激的葡萄糖摄取,表明脂肪细胞可能在分化的 3T3-L1 脂肪细胞中抑制 DGAT1 后提高胰岛素敏感性。
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