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T863

Chemical Structure : T863

CAS No.: 701232-20-4

T863 (DGAT1 inhibitor T863)

Catalog No.: 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.

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Biological Activity

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.

Physicochemical Properties

M.Wt 394.4668
Formula C22H26N4O3
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

Cyclohexaneacetic acid, 4-[4-(4-amino-7,7-dimethyl-7H-pyrimido[4,5-b][1,4]oxazin-6-yl)phenyl]-, trans-

References

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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