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Purity: ≥98%
Atglistatin is a highly potent and selective inhibitor of adipose triglyceride lipase (ATGL) with IC50 of 0.7 μM, it showed high selectivity over other key metabolic lipases. 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%.
| ln Vitro |
Triacylglycerol (TG) hydrolase activity in wild-type white adipose tissue (WAT) is inhibited by atglistatin in a dose-dependent manner; at the maximum concentration, this inhibition reaches 78%. When compared to wild-type preparations, the TG hydrolase activity in WAT lysates from ATGL-ko mice was roughly 70% lower, while atglistatin only moderately affected the residual activity. The TG hydrolase activity of WAT was nearly completely inhibited (-95%) by the combination of atglistatin and the hormone-sensitive lipase (HSL) inhibitor Hi 76-0079, indicating that HSL is primarily responsible for the majority of the non-ATGL activity[1].
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| ln Vivo |
Animals were given oral gavages with dissolved agostatin in olive oil. Following application, tissue and blood were taken in order to measure the inhibitor concentrations, tissue triacylglycerol (TG) levels, and plasma parameters. Fatty acids (FA) and glycerol, the lipolytic parameters, dropped at 4 and 8 hours after application and recovered to normal after 12 hours, according to time course experiments. Eight hours after treatment, there was a dose-dependent drop in FA and glycerol levels of up to 50% and 62%, respectively. Additionally, atglistatin significantly reduced plasma TG levels (-43%) while having no discernible effect on blood sugar, total cholesterol, ketone bodies, or insulin levels. Intraperitoneal injection of Atglistatin was likewise found to inhibit lipolysis in a dose- and time-dependent manner [1].
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| References |
[1]. Mayer N, et al. Development of small-molecule inhibitors targeting adipose triglyceride lipase. (2013) Nat Chem Biol. 9(12):785-7
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| Molecular Formula |
C17H21N3O
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| Molecular Weight |
283.37
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| CAS # |
1469924-27-3
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| Related CAS # |
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| SMILES |
O=C(N(C([H])([H])[H])C([H])([H])[H])N([H])C1=C([H])C([H])=C([H])C(=C1[H])C1C([H])=C([H])C(=C([H])C=1[H])N(C([H])([H])[H])C([H])([H])[H]
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| InChi Key |
AWOPBSAJHCUSAS-UHFFFAOYSA-N
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| InChi Code |
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)
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| Chemical Name |
3-(4-(dimethylamino)-[1,1-biphenyl]-3-yl)-1,1-dimethylurea
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| Synonyms |
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.82 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (8.82 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. View More
Solubility in Formulation 3: 6.25 mg/mL (22.06 mM) in Corn Oil (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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