T863

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[1][2].

Product Specifications

CAS Number

[701232-20-4]

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Acyltransferase

Type

Reference compound

Related Pathways

Metabolic Enzyme/Protease

Applications

Metabolism-sugar/lipid metabolism

Field of Research

Metabolic Disease

Assay Protocol

https://www.medchemexpress.com/T863.html

Purity

99.83

Solubility

DMSO : ≥ 50 mg/mL

Smiles

O=C(O)C[C@H]1CC[C@H](C2=CC=C(C3=NC4=C(N)N=CN=C4OC3(C)C)C=C2)CC1

Molecular Formula

C22H26N4O3

Molecular Weight

394.47

Precautions

H302, H315, H319, H335

References & Citations

[1]Cao J, 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]Alan M Birch, et al. Discovery of a potent, selective, and orally efficacious pyrimidinooxazinyl bicyclooctaneacetic acid diacylglycerol acyltransferase-1 inhibitor. J Med Chem. 2009 Mar 26;52 (6) :1558-68.