SR 1664

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Cat.No. 4409 - SR 1664 | C33H29N3O5 | CAS No. 1338259-05-4
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% (HPLC)
Datasheet
Citations
Reviews
Literature (4)

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

M. Wt 547.6
Formula C33H29N3O5
Storage Store at -20°C
Purity ≥97% (HPLC)
CAS Number 1338259-05-4
PubChem ID 53239854
InChI Key IIJDFXNUWZTHIM-NRFANRHFSA-N
Smiles CC2=C(C)N(CC3=CC=C(C4=CC=CC=C4C(O)=O)C=C3)C1=CC=C(C(N[C@H](C5=CC=C([N+]([O-])=O)C=C5)C)=O)C=C12

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.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 54.76 100
ethanol 54.76 100

Preparing Stock Solutions

The following data is based on the product molecular weight 547.6. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.83 mL 9.13 mL 18.26 mL
5 mM 0.37 mL 1.83 mL 3.65 mL
10 mM 0.18 mL 0.91 mL 1.83 mL
50 mM 0.04 mL 0.18 mL 0.37 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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References

References are publications that support the biological activity of the product.

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, SR 1664 supplier, SR1664, antidiabetics, diabetes, PPARgamma, PPARg, peroxisome, proliferator, activated, receptor, ligand, Cdk5, phosphorylation, LBD, Receptors, 4409, Tocris Bioscience

Citations for SR 1664

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