SR 1664

Catalog # Availability Size / Price Qty
4409/10
4409/50
Cat.No. 4409 - SR 1664 | C33H29N3O5 | CAS No. 1338259-05-4
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Description: High affinity PPARγ ligand; blocks Cdk5-dependent PPARγ phosphorylation

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

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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

Formula:
C33H29N3O5
Solubility:
Soluble to 100 mM in DMSO and to 100 mM in ethanol
Storage:
Store the unopened product at -20 to -70 °C. Use a manual defrost freezer and avoid repeated freeze-thaw cycles. Do not use past expiration date.
CAS No:
1338259-05-4

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.

Background References

  1. A second chance for a PPARγ targeted therapy?
    Norris and Sigmund
    Circ.Res., 2012;110:8
  2. Antidiabetic actions of a non-agonist PPARγ ligand blocking Cdk5-mediated phosphorylation.
    Choi et al.
    Nature, 2011;477:477

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