Chemical Structure : T863
CAS No.: 701232-20-4
货号: PC-45795Not For Human Use, Lab Use Only.
T-863 is a potent and selective, cell-permeable DGAT1 inhibitor that binds to the oleoyl-CoA binding pocket of DGAT1 with IC50 of 17 nM in TLC assay.
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
10 mg | ¥1280 | In stock | |
25 mg | ¥2180 | In stock | |
50 mg | ¥3580 | In stock | |
100 mg | Get quote |
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T863 is a potent and selective, cell-permeable DGAT1 inhibitor that binds to the oleoyl-CoA binding pocket of DGAT1 with IC50 of 17 nM in TLC assay.
T863 shows no inhibitory activity against hMGAT3, hDGAT2, and hMGAT2 at >10 uM.
T863 inhibits DGAT1-mediated triacylglycerol formation in HEK293-DGAT1 cells (IC50=122 nM).
T863 causes weight loss, reduces serum and liver triglycerides, improves insulin sensitivity, and lowers serum cholesterol in diet-induced obese mice.
T863 is orally bioavailable.
分子量 | 394.4668 | |
分子式 | C22H26N4O3 | |
外观性状 | Solid | |
储存条件 |
|
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Solubility |
10 mM in DMSO |
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Chemical Name/SMILES |
Cyclohexaneacetic acid, 4-[4-(4-amino-7,7-dimethyl-7H-pyrimido[4,5-b][1,4]oxazin-6-yl)phenyl]-, trans- |
1. Cao J, et al. J Biol Chem. 2011 Dec 2;286(48):41838-51.
2. Tuohetahuntila M, et al. J Lipid Res. 2016 Jul;57(7):1162-74.
3. Dow RL, et al. Bioorg Med Chem Lett. 2011 Oct 15;21(20):6122-5.
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