Atglistatin |
| رقم الكتالوجGC15770 |
Atglistatin هو مثبط انتقائي للليباز ثلاثي الجليسريد الدهني (ATGL) الذي يثبط تحلل الدهون باستخدام IC50 من 0.7 ميكرومتر في المختبر
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1469924-27-3
Sample solution is provided at 25 µL, 10mM.
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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.
| Kinase experiment [1]: | |
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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 experiment [1]: | |
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Cell lines |
3T3-L1 fibroblasts, AML-12 mouse hepatocytes |
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Preparation method |
The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
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Reacting condition |
0.1, 1, 10, or 50 μM for 1-3 h |
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Applications |
Atglistatin showed highest adipose triglyceride lipase (ATGL) inhibition potential with IC50 value of 0.7 μM. Atglistatin was highly effective in inhibiting lipolysis in 3T3-L1 adipocytes and white adipose tissue (WAT) organ cultures of wild-type mice by targeting ATGL. |
| Animal experiment [1]: | |
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Animal models |
Mice (C57Bl/6J) model |
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Dosage form |
200 μmol/kg; oral gavage or intraperitoneal administration, for 8 h; |
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Applications |
Atglistatin showed the potential of inhibiting lipolysis in fasted wild-type C57Bl/6J mice. Atglistatin also caused a strong reduction in plasma triacylglycerol (TG) levels (-43%). |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: 1.Mayer, N., Schweiger, M., Romauch, M., Grabner, G. F., Eichmann, T. O., Fuchs, E., Ivkovic, J., Heier, C., Mrak, I., Lass, A., Hofler, G., Fledelius, C., Zechner, R., Zimmermann, R. and Breinbauer, R. (2013) Development of small-molecule inhibitors targeting adipose triglyceride lipase. Nat Chem Biol. 9, 785-787 |
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| Cas No. | 1469924-27-3 | SDF | |
| Chemical Name | 3-[3-[4-(dimethylamino)phenyl]phenyl]-1,1-dimethylurea | ||
| Canonical SMILES | CN(C)C1=CC=C(C=C1)C2=CC(=CC=C2)NC(=O)N(C)C | ||
| Formula | C17H21N3O | M.Wt | 283.37 |
| الذوبان | ≥ 14.15mg/mL in DMSO | Storage | Store at -20° C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.529 mL | 17.6448 mL | 35.2896 mL |
| 5 mM | 0.7058 mL | 3.529 mL | 7.0579 mL |
| 10 mM | 0.3529 mL | 1.7645 mL | 3.529 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 4 reference(s) in Google Scholar.)
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