AtglistatinATGL inhibitor, potent and selective CAS# 1469924-27-3 |
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Quality Control & MSDS
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Chemical structure
3D structure
| Cas No. | 1469924-27-3 | SDF | Download SDF |
| PubChem ID | 71699712 | Appearance | Powder |
| Formula | C17H21N3O | M.Wt | 283.37 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | DMSO : ≥ 100 mg/mL (352.90 mM) H2O : < 0.1 mg/mL (insoluble) *"≥" means soluble, but saturation unknown. | ||
| Chemical Name | 3-[3-[4-(dimethylamino)phenyl]phenyl]-1,1-dimethylurea | ||
| SMILES | CN(C)C1=CC=C(C=C1)C2=CC(=CC=C2)NC(=O)N(C)C | ||
| Standard InChIKey | AWOPBSAJHCUSAS-UHFFFAOYSA-N | ||
| Standard 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) | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | Atglistatin is a selective adipose triglyceride lipase (ATGL) inhibitor with IC50 of 0.7 μM for lipolysis in vitro.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].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]. References: | |||||
Atglistatin Dilution Calculator
Atglistatin Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 3.529 mL | 17.6448 mL | 35.2896 mL | 70.5791 mL | 88.2239 mL |
| 5 mM | 0.7058 mL | 3.529 mL | 7.0579 mL | 14.1158 mL | 17.6448 mL |
| 10 mM | 0.3529 mL | 1.7645 mL | 3.529 mL | 7.0579 mL | 8.8224 mL |
| 50 mM | 0.0706 mL | 0.3529 mL | 0.7058 mL | 1.4116 mL | 1.7645 mL |
| 100 mM | 0.0353 mL | 0.1764 mL | 0.3529 mL | 0.7058 mL | 0.8822 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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Atglistatin is a potent and selective inhibitor of ATGL with IC50 value of 0.7 μM [1].
Adipose triglyceride lipase (ATGL) is a rate-limiting enzyme in the mobilization of fatty acids from cellular triglyceride stores. Deregulated fatty acid metabolism may lead to metabolic disorders and dyslipidemic [1].
Atglistatin is a potent and selective ATGL inhibitor. In lysates from E. coli overexpressing ATGL, atglistatin inhibited ATGL activity with IC50 value of 0.7 μM. Atglistatin at concentrations up to 50 μM had no cytotoxicity. Also, atglistatin inhibited ATGL with Ki value of 355 nM in a competitive way. In white adipose tissue (WAT) lysates of wild-type mice, atglistatin inhibited triacylglycerol (TG) hydrolase activity by 78%. The combination of Atglistatin and the HSL inhibitor Hi 76-007917 inhibited TG hydrolase activity by 95%. In WAT cultures of wild-type mice, atglistatin reduced FA and glycerol release up to 72% and 62% respectively in the presence of forskolin [1].
In fasted wild-type C57Bl/6J mice, atglistatin inhibited lipolysis in a dose- and time-dependent way. Atglistatin reduced plasma TG levels by 43% and decreased glycerol and FA levels up to 62% and 50% respectively in a dose dependent way [1].
Reference:
[1]. Mayer N, Schweiger M, Romauch M, et al. Development of small-molecule inhibitors targeting adipose triglyceride lipase. Nat Chem Biol, 2013, 9(12): 785-787.
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New Atglistatin closely related analogues: Synthesis and structure-activity relationship towards adipose triglyceride lipase inhibition.[Pubmed:27155760]
Eur J Med Chem. 2016 Aug 8;118:290-8.
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.
