SR 1664

Cat. No. 4409

SR 1664 C33H29N3O5 [1338259-05-4]

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Chemical Name: 4'-[[2,3-Dimethyl-5-[[[(1S)-1-(4-nitrophenyl)ethyl]amino]carbonyl]-1H-indol-1-yl]methyl]-[1,1'-biphenyl]-2-carboxylic acid

Biological Activity

Antidiabetic agent; binds to PPARγ and potently inhibits Cdk5-mediated PPARγ phosphorylation (IC50 = 80 nM; Ki = 28.67 nM) without exhibiting PPARγ agonist activity. Does not inhibit Cdk5-dependent phosphorylation of Rb. Reduces fasting insulin levels and improves insulin sensitivity in a mouse model of diabetes.

Technical Data

Soluble to 100 mM in DMSO and to 100 mM in ethanol
>97 %
Store at -20°C

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.

Certificate of Analysis / Safety Data Sheet

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Norris and Sigmund (2012) A second chance for a PPARγ targeted therapy? Circ.Res. 110 8. PMID: 22223206.

Choi et al (2011) Antidiabetic actions of a non-agonist PPARγ ligand blocking Cdk5-mediated phosphorylation. Nature 477 477. PMID: 21892191.

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Keywords: SR 1664, supplier, SR1664, antidiabetics, diabetes, PPARgamma, PPARg, peroxisome, proliferator, activated, receptor, ligand, Cdk5, phosphorylation, LBD, Tocris Bioscience, PPARγ products

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