[CAS NO. 1469924-27-3] Atglistatin
PRODUCTS SPECIFICATIONS [1469924-27-3]
DESCRIPTION [1469924-27-3]
Overview
| MDL | MFCD28009494 |
|---|---|
| Molecular Weight | 283.37 |
| Molecular Formula | C17H21N3O |
| SMILES | O=C(NC1=CC(C2=CC=C(N(C)C)C=C2)=CC=C1)N(C)C |
8 Publications Citing Use of MCE
- [1]Cell Metab. 2022 Aug 11;S1550-4131(22)00310-2.
- [2]Neuron. 2020 Jan 22;105(2):276-292.e5.
- [3]Nat Commun. 2022 Nov 2;13(1):6577.
- [4]Diabetologia. 2022 Jan 12.
- [5]J Biomed Sci. 2020 Sep 1;27(1):91.
- [6]Biochim Biophys Acta Mol Cell Biol Lipids. 2021 Jun 7;158988.
- [7]Fish Physiol Biochem. 2021 Feb;47(1):173-188.
- [8]Fish Physiol Biochem. 2017 Jun;43(3):813-822.
Summary
Atglistatin is a selective adipose triglyceride lipase ( ATGL ) inhibitor which inhibits lipolysis with an IC 50 of 0.7 μM in vitro .
IC50 & Target
IC50: 0.7 μM (ATGL) [1]
In Vitro
Atglistatin inhibits Triacylglycerol (TG) hydrolase activity of wild-type white adipose tissue (WAT) in a dose-dependent manner up to 78% at the highest concentration. In comparison to wild-type preparations, TG hydrolase activity in WAT lysates from ATGL-ko animals is reduced by approximately 70% and Atglistatin had only a moderate effect on the residual activity. The combined use of Atglistatin and the hormone-sensitive lipase (HSL) inhibitor Hi 76-0079 leads to an almost complete inhibition (-95%) of TG hydrolase activity of WAT which implicates that most of the non-ATGL activity can be ascribed to HSL [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Animals receive Atglistatin dissolved in olive oil by oral gavage. After application, blood and tissues are collected for determination of plasma parameters, tissue Triacylglycerol (TG) levels, and inhibitor concentrations. Time-course experiments revealed that the lipolytic parameters fatty acids (FA) and glycerol are reduced 4 and 8 hours after application and returned to normal after 12 hours. Eight hours after treatment, a dose-dependent decrease is observed in FA and glycerol levels up to 50% and 62%, respectively. Atglistatin also caused a strong reduction in plasma TG levels (-43%) while blood glucose, total cholesterol, ketone bodies, and insulin levels do not significantly change. Dose and time-dependent inhibition of lipolysis is also observed in response to intraperitoneal injection of Atglistatin [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : ≥ 100 mg/mL ( 352.90 mM )
* "≥" means soluble, but saturation unknown.
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 3.5290 mL | 17.6448 mL | 35.2896 mL |
| 5 mM | 0.7058 mL | 3.5290 mL | 7.0579 mL |
| 10 mM | 0.3529 mL | 1.7645 mL | 3.5290 mL |