Conditionnement : 5mg
Téléphone : +1 850 650 7790
Synonyms:
| Description | Atglistatin is a highly effective, specific and competitive ATGL inhibitor with an IC50 of ~0.7 μM for inhibition of lipolysis in vitro, and no toxicity when the concentration up to 50 μM. |
| Targets & IC50 | ATGL:0.7 μM |
| In vitro | Atglistatin inhibits ATGL, consequently suppressing lipid breakdown in both cellular and organ cultures without exhibiting cytotoxic effects at concentrations up to 50 µM. |
| In vivo | Atglistatin, administered orally (p.o.), reduces fatty acids (FA) and glycerol by up to 50% and 62% respectively, in a dose-dependent manner, and also significantly reduces triglyceride (TG) levels in the plasma by 43%. When administered via intraperitoneal injection (i.p.), Atglistatin inhibits lipolysis in a dose- and time-dependent manner. Moreover, Atglistatin exhibits significant differences in tissue distribution, primarily accumulating in the liver and adipose tissue. |
| Kinase Assay | Determination of lipase activity: For determination of lipase activity, lysates are incubated with a substrate containing radiolabeled [9,10-3H(N)]-triolein. Subsequently, FA are extracted and quantitated by liquid scintilation counting. Data are presented as mean S.D. of triplicate determinations and representative for at least three independent experiments. |
| Cell Research | For MTT-based in vitro viability assays, cells are seeded in 96-well plates and cultured under standard conditions for 24 h. The next day, cells are pretreated with different concentrations of Atglistatin dissolved in DMSO or Cisplatin dissolved in DMF as positive control for 2 h. Medium is replaced by an identical fresh medium and incubated again for the indicated time points. Thereafter, cells are incubated for 3 h with 100 μL Thiazolyl Blue Tetrazolium Bromide (MTT). The resulting violet formazan crystals are dissolved by adding 100 μL of MTT solubilization solution (0.1% NP-40, 4 mM HCl and anhydrous isopropanol). After complete dissolution of the formazan product, absorbance is measured at 595 nm using 690 nm as reference wavelength.(Only for Reference) |
| Molecular Weight | 283.37 |
| Formula | C17H21N3O |
| Cas No. | 1469924-27-3 |
| Smiles | CN(C)C(=O)Nc1cccc(c1)-c1ccc(cc1)N(C)C |
| Relative Density. | 1.135 g/cm3 (Predicted) |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. | ||||||||||||||||||||||||||||||||||||||||
| Solubility Information | H2O: < 1 mg/mL (insoluble or slightly soluble) DMSO: 100 mg/mL (352.9 mM), Sonication is recommended.  Ethanol: 4 mg/mL (14.12 mM), Sonication is recommended. | ||||||||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 4 mg/mL (14.12 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | ||||||||||||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||||||||||||
Ethanol/DMSO
DMSO
Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density. | |||||||||||||||||||||||||||||||||||||||||
For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 
10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO stock solution to 400 µL PEG300 and mix thoroughly until the solution becomes clear.
2) Add 50 µL Tween 80 and mix well until fully clarified.
3) Add 450 µL Saline,PBS or ddH2O and mix thoroughly until a homogeneous solution is obtained.
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