1469924-27-3

Basic information

• Product Name: Atglistatin
• Synonyms: Atglistatin;N'-[4'-(Dimethylamino)[1,1'-biphenyl]-3-yl]-N,N-dimethylurea;3-(4'-(dimethylamino)-[1,1'-biphenyl]-3-yl)-1,1-dimethylurea;Atglistatin N'-[4'-(Dimethylamino)[1,1'-biphenyl]-3-yl]-N,N-dimethylurea;N'-[4'-(Dimethylamino)[1,1'-biphenyl]-3-yl]-N,N-dimethylurea Atglistatin;Atglistatin, >=98%
• CAS NO: 1469924-27-3
• Molecular Formula: C17H21N3O
• Molecular Weight: 283.36814
• EINECS: 200-256-5
• Product Categories: Inhibitors
• Mol File: 1469924-27-3.mol
• Article Data: 0

Chemical Properties

• Boiling Point: 498.6±45.0 °C(Predicted)
• Appearance: /
• Density: 1.135±0.06 g/cm3(Predicted)
• Storage Temp.: 2-8°C
• Solubility: Soluble in DMSO (up to 5 mg/ml) or in Ethanol (up to 5 mg/ml with warming)
• PKA: 15.01±0.70(Predicted)
• Stability: Stable for 2 years as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 3 months.
• CAS DataBase Reference: Atglistatin(CAS DataBase Reference)
• NIST Chemistry Reference: Atglistatin(1469924-27-3)
• EPA Substance Registry System: Atglistatin(1469924-27-3)

Safety Data

• Hazard Codes: Xn
• Statements: 22-36/37/38
• Safety Statements: 36/37/39
• Hazardous Substances Data: 1469924-27-3(Hazardous Substances Data)

Usage

Description

Atglistatin is a potent, selective, and competitive inhibitor of adipose triglyceride lipase (ATGL or PNPLA2), a key enzyme involved in the initial step of triglyceride hydrolysis in adipocyte and non-adipocyte lipid droplets. It effectively blocks lipolysis by ATGL both in vitro and in vivo without affecting other lipases or lysophospholipases.

Uses

Used in Pharmaceutical Industry:
Atglistatin is used as a selective inhibitor of ATGL for its potential therapeutic applications in managing lipid metabolism and related disorders. By specifically targeting ATGL, it can help regulate the breakdown of triglycerides and control the release of fatty acids, which may have implications in treating conditions such as obesity, diabetes, and cardiovascular diseases.
Used in Research Applications:
Atglistatin is also utilized as a research tool in the field of biochemistry and molecular biology. It aids in studying the role of ATGL in lipid metabolism, lipolysis, and the overall understanding of energy homeostasis and lipid storage in cells. This selective inhibition can provide valuable insights into the development of novel therapeutic strategies for various metabolic disorders.

Biochem/physiol Actions

Atglistatin is the first selective inhibitor of adipose triglyceride lipase (ATGL), the rate limiting enzyme involved in the mobilization of fatty acids from cellular triglyceride stores. Atglistatin has an IC50 of 0.7 μM in E.coli and no activity against monoglycerol lipase (MGL), hormone-sensitive lipase (HSL), or pancreatic lipase and lipoprotein lipase PNPLA6 and PNPLA7. ATGL generates diacylglycerol from cellular triglyceride stores, which is then degraded by hormone-sensitive lipase (HSL) and monoglyceride lipase into glycerol and fatty acids, promoting the synthesis of lipotoxic metabolites that have been associated with the development of insulin resistance. Atglistatin inhibition of ATGL has been shown to reduce fatty acid mobilization in vitro and in vivo.

References

1) Mayer et al. (2013), Development of small-molecule inhibitors targeting adipose triglyceride lipase; Nat. Chem. Biol. 9 785 2) Zagani et al. (2015) Inhibition of adipose triglyceride lipase (ATGL) by the putative tumor suppressor G0S2 or a small molecule inhibitor attenuates the growth of cancer cells; Oncotarget 6 28282