SML0539

T863

≥98% (HPLC)

• Synonym(s): 2-((1,4-trans)-4-(4-(4-Amino-7,7-dimethyl-7H-pyrimido[4,5-b][1,4]oxazin-6-yl)- phenyl)cyclohexyl)acetic acid, T-863, trans-4-[4-(4-Amino-7,7-dimethyl-7H-pyrimido[4,5-b][1,4]oxazin-6-yl)phenyl]-cyclohexaneacetic acid
• Empirical Formula (Hill Notation): C₂₂H₂₆N₄O₃
• CAS Number: 701232-20-4
• Molecular Weight: 394.47
• MDL number: MFCD11977270
• UNSPSC Code: 51111800
• PubChem Substance ID: 329825541
• NACRES: NA.77

Properties

• Assay: ≥98% (HPLC)
• form: powder
• color: white to beige
• solubility: DMSO: 15 mg/mL (clear solution)
• storage temp.: 2-8°C
• SMILES string: CC1(C)Oc2ncnc(N)c2N=C1c3ccc(cc3)[C@@H]4CC[C@H](CC4)CC(O)=O
• InChI: 1S/C22H26N4O3/c1-22(2)19(26-18-20(23)24-12-25-21(18)29-22)16-9-7-15(8-10-16)14-5-3-13(4-6-14)11-17(27)28/h7-10,12-14H,3-6,11H2,1-2H3,(H,27,28)(H2,23,24,25)/t13-,14-
• InChI key: FUIYMYNYUHVDPT-HDJSIYSDSA-N

Description

Application

T863 has been used as a diglyceride acyltransferase (DGAT1) inhibitor:

• to provide the opportunity to precisely control the DGAT inhibition
• to treat mouse embryonic fibroblasts (MEFs) to analyse lipid droplet biogenesis
• to specifically block neutral lipid synthesis and lipid droplet formation in HT-1080 cells
• to block lipid droplet (LD) formation

Biochem/physiol Actions

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. T863 causes weight loss, reduction in serum and liver triglycerides, and improved insulin sensitivity in obese mice.

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable