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SR1664

🥰Excellent
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

🥰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 SizePriceAvailabilityQuantity
1 mg45 €In Stock
2 mg64 €In Stock
5 mg107 €In Stock
10 mg139 €In Stock
25 mg305 €In Stock
50 mg543 €In Stock
100 mg780 €In Stock
500 mg1.605 €In Stock
1 mL x 10 mM (in DMSO)118 €In Stock
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Purity:98.02%
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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].
AliasSR 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.
Solubility Information
DMSO: 60 mg/ml (109.57 mM)
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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