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SR1664

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Catalog No. T23389Cas No. 1338259-05-4
Alias SR 1664

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.

SR1664

SR1664

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🥰Excellent
Purity: 98.02%
Catalog No. T23389Alias SR 1664Cas No. 1338259-05-4
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 SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$48In StockIn Stock
2 mg$68In StockIn Stock
5 mg$113In StockIn Stock
10 mg$147In StockIn Stock
25 mg$298In StockIn Stock
50 mg$433In StockIn Stock
100 mg$621In StockIn Stock
200 mg$877In StockIn Stock
1 mL x 10 mM (in DMSO)$125In StockIn Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
This molecule is a custom-made product. TargetMol has an excellent synthesis team with the experience and capability to provide you with cost-effective products.If you have any questions, please feel free to contact us. We are committed to serving you wholeheartedly.
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.
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Purity:98.02%
Appearance:Solid
Color:Yellow
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Product Introduction

Bioactivity
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].
SynonymsSR 1664
Chemical Properties
Molecular Weight547.6
FormulaC33H29N3O5
Cas No.1338259-05-4
SmilesC[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)
Storage & Solubility Information
StoragePowder: -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
1mg5mg10mg50mg
1 mM1.8262 mL9.1308 mL18.2615 mL91.3075 mL
5 mM0.3652 mL1.8262 mL3.6523 mL18.2615 mL
10 mM0.1826 mL0.9131 mL1.8262 mL9.1308 mL
20 mM0.0913 mL0.4565 mL0.9131 mL4.5654 mL
50 mM0.0365 mL0.1826 mL0.3652 mL1.8262 mL
100 mM0.0183 mL0.0913 mL0.1826 mL0.9131 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent 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.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent 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 ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
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μL
2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

Dose Conversion

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc

Keywords

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