Atglistatin

• CAT Number: I001787
• CAS Number: 1469924-27-3
• Molecular Formula: C₁₇H₂₁N₃O
• Molecular Weight: 283.37
• Purity: ≥95%
• Target: ATGL
• Solubility: DMSO: ≥ 45 mg/mL
• Storage: -20°C
• IC50: 0.7 uM [1]
• InChI: InChI=1S/C17H21N3O/c1-19(2)16-10-8-13(9-11-16)14-6-5-7-15(12-14)18-17(21)20(3)4/h5-12H,1-4H3,(H,18,21)
• InChIKey: AWOPBSAJHCUSAS-UHFFFAOYSA-N
• SMILES: CN(C)C1=CC=C(C=C1)C2=CC(=CC=C2)NC(=O)N(C)C

Atglistatin(CAT: I001787) is a highly potent, selective, and competitive inhibitor of adipose triglyceride lipase (ATGL). ATGL is an enzyme involved in the breakdown of triglycerides into fatty acids, playing a crucial role in lipid metabolism. By inhibiting ATGL, Atglistatin can prevent the hydrolysis of triglycerides and the release of fatty acids from adipose tissue. This inhibition may have implications for metabolic disorders, such as obesity and dyslipidemia.

Reference

1:Eur J Med Chem. 2016 Aug 8;118:290-8. doi: 10.1016/j.ejmech.2016.04.021. Epub 2016 Apr 10. New Atglistatin closely related analogues: Synthesis and structure-activity relationship towards adipose triglyceride lipase inhibition.Roy PP,D/’Souza K,Cuperlovic-Culf M,Kienesberger PC,Touaibia M, PMID: 27155760 DOI: 10.1016/j.ejmech.2016.04.021 Abstract: Adipose Triglyceride Lipase (ATGL) performs the first and rate-limiting step in lipolysis by hydrolyzing triacylglycerols stored in lipid droplets to diacylglycerols. By mediating lipolysis in adipose and non-adipose tissues, ATGL is a major regulator of overall energy metabolism and plasma lipid levels. Since chronically high levels of plasma lipids are linked to metabolic disorders including insulin resistance and type 2 diabetes, ATGL is an interesting therapeutic target. In the present study, fourteen closely related analogues of Atglistatin (1), a newly discovered ATGL inhibitor, were synthesized, and their ATGL inhibitory activity was evaluated. The effect of these analogues on lipolysis in 3T3-L1 adipocytes clearly shows that inhibition of the enzyme by Atglistatin (1) is due to the presence of the carbamate and N,N-dimethyl moieties on the biaryl central core at meta and para position, respectively. Mono carbamate-substituted analogue C2, in which the carbamate group was in the meta position as in Atglistatin (1), showed slight inhibition. Low dipole moment of Atglistatin (1) compared to the synthesized analogues possibly explains the lower inhibitory activities. Copyright © 2016 Elsevier Masson SAS. All rights reserved.