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SR1664 is a potent and selective PPARγ inhibitor with potential antidiabetic activity. SR1664 binds to PPARγ and potently inhibits Cdk5-mediated PPARγ phosphorylation (IC50 = 80 nM; Ki = 28.67 nM) without exhibiting PPARγ agonist activity.

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $48 | In Stock | In Stock | |
| 2 mg | $68 | In Stock | In Stock | |
| 5 mg | $113 | In Stock | In Stock | |
| 10 mg | $147 | In Stock | In Stock | |
| 25 mg | $322 | In Stock | In Stock | |
| 50 mg | $572 | In Stock | In Stock | |
| 100 mg | $822 | In Stock | In Stock | |
| 500 mg | $1,690 | Backorder | Backorder | |
| 1 mL x 10 mM (in DMSO) | $125 | In Stock | In Stock |
| Description | SR1664 is a potent and selective PPARγ inhibitor with potential antidiabetic activity. SR1664 binds to PPARγ and potently inhibits Cdk5-mediated PPARγ phosphorylation (IC50 = 80 nM; Ki = 28.67 nM) without exhibiting PPARγ agonist activity. |
| Targets&IC50 | PPARγ:28.67 nM(Ki), PPARγ:80 nM |
| In vitro | Mutagenesis of F282 to alanine (F282A) altered the pharmacology of SR1664 on PPARγ activity, acting as an agonist of the mutant receptor in a transcriptional activity assay, and differentially displacing nuclear receptor co-repressor 1. Together these results suggest that SR1664 actively antagonizes PPARγ through a stereo-specific AF2-mediated, F282-dependent clash, and that stereospecificity confers antagonism within the biaryl indole scaffold[1]. |
| Synonyms | SR 1664 |
| Molecular Weight | 547.6 |
| Formula | C33H29N3O5 |
| Cas No. | 1338259-05-4 |
| Smiles | C[C@H](NC(=O)c1ccc2n(Cc3ccc(cc3)-c3ccccc3C(O)=O)c(C)c(C)c2c1)c1ccc(cc1)[N+]([O-])=O |
| Relative Density. | 1.27 g/cm3 (Predicted) |
| Color | Yellow |
| Appearance | Solid |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 60 mg/mL (109.57 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (3.65 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 | ||||||||||||||||||||||||||||||||||||
DMSO
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