CAY10599A TZD that is a PPARγ agonist

CAY10599 (CAS 1143573-33-4)

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Synonym: 2-[[1-[3-[4-([1,1'-biphenyl]-4-ylcarbonyl)-2-propylphenoxy]propyl]-1,2,3,4-tetrahydro-5-quinolinyl]oxy]-2-methyl-propanoic acid
Application: A TZD that is a PPARγ agonist
CAS Number: 1143573-33-4
Purity: ≥98%
Molecular Weight: 591.75
Molecular Formula: C38H41NO5
* Refer to Certificate of Analysis for lot specific data (including water content).
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CAY10599 is a PPARγ agonist that is 4-fold more potent than rosiglitazone at PPARγ demonstrating an EC50 value of 0.05 μM. This compound shows high selectivity for the PPARγ receptor over PPARβ (EC50 > 10 μM) or PPARα (EC50 = 3.99 μM).


References

1 Willson, T.M., Cobb, J.E., Cowan, D.J., et al. The structure-activity relationship between peroxisome proliferator-activated receptor γ agonism and the antihyperglycemic activity of thiazolidinediones. J Med Chem 39 665-668 (1996). 2 Cantello, B.C.C., Cawthorne, M.A., Cottam, G.P., et al. [[ω-(Heterocyclylamino)alkoxy]benzyl]-2,4-thiazolidinediones as potent antihyperglycemic agents. J Med Chem 37 3977-3985 (1994). 3 Lin, C., Peng, Y., Coumar, M.S., et al. Design and structural analysis of novel pharmacophores for potent and selective peroxisome proliferator-activated receptor g agonists. J Med Chem 52 2618-2622 (2009).

Physical State :
Solid
Solubility :
Soluble in ethanol (~25 mg/ml), DMSO (~25 mg/ml), and DMF (~25 mg/ml).
Storage :
Store at -20° C
Boiling Point :
~789.0° C at 760 mmHg (Predicted)
Density :
~1.2 g/cm3 (Predicted)
Refractive Index :
n20D 1.59 (Predicted)
IC50 :
PPARγ: EC5050 = 50 nM (human); PPARα: EC5050 = 3.99 µM (human); PPARδ: EC5050 >10 µM (human)
pK Values :
pKa: 3.31 (Predicted), pKb: 5.36 (Predicted)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
PubChem CID :
42626030
MDL Number :
MFCD18382106
SMILES :
CC(C)(C(O)=O)OC1=CC=CC2=C1CCCN2CCCOC3=CC=C(C(C4=CC=C(C5=CC=CC=C5)C=C4)=O)C=C3CCC

Download SDS (MSDS)

Certificate of Analysis

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