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SR 1664

Catalog #: 4409 Datasheet / COA / SDS

Discontinued Product

4409 has been discontinued.
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SR 1664 | CAS No. 1338259-05-4 | Additional PPAR gamma Receptor Products
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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

Purity: ≥97%

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Biological Activity

SR 1664 is an 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

M.Wt:
547.6
Formula:
C33H29N3O5
Solubility:
Soluble to 100 mM in DMSO and to 100 mM in ethanol
Purity:
≥97%
Storage:
Store at -20°C
CAS No:
1338259-05-4

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

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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