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SR 202 Catalog No.GC11586

PPAR antagonist

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Sample solution is provided at 25 µL, 10mM.

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Chemical Properties

Cas No. 76541-72-5 SDF
Chemical Name (S)-(4-chlorophenyl)(dimethoxyphosphoryl)methyl dimethyl phosphate
Canonical SMILES ClC1=CC=C(C=C1)[C@@H](OP(OC)(OC)=O)P(OC)(OC)=O
Formula C11H17ClO7P2 M.Wt 358.65
Solubility Water: 100 mM Storage Desiccate at RT
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
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IC50: 140 μM for attenuation of troglitazone-induced peroxisome proliferator-activated receptor gamma (PPAR) transcriptional activity [1]

The phosphonophosphate SR-202 [(S)-(4-chlorophenyl)(dimethoxyphosphoryl)methyl dimethyl phosphate] is a PPAR antagonist, which inhibits both TZD-stimulated recruitment of the coactivator steroid receptor coactivator-1 and TZD-induced transcriptional activity of the receptor. PPAR is a nuclear receptor which regulates glucose metabolism and fatty acid storage.

In vitro: SR-202 is a specific antagonist of PPAR, which shows selectivity both among the PPAR family members and other nuclear receptors. SR-202 also Inhibits PPAR-dependent differentiation of adipocytes. In cell culture, SR-202 efficiently antagonizes hormone- and TZD induced adipocyte differentiation [1].

In vivo:. Decreasing PPAR activity by treatment with SR-202 leads to a reduction of both high fat diet-induced adipocyte hypertrophy and insulin resistance. Treatment with SR-202 also dramatically improves insulin sensitivity in the diabetic ob/ob mice [1]. When wild-type mice are fed a high-fat diet, the plasma levels of TNF-α are raised, and SR-202 treatment protects against this rise [2]..

Clinical trial: So far, no clinical study has been conducted.

[1] Rieusset J, Touri F, Michalik L, Escher P, Desvergne B, Niesor E, Wahli W.  A new selective peroxisome proliferator-activated receptor gamma antagonist with antiobesity and antidiabetic activity. Mol Endocrinol. 2002 Nov;16(11):2628-44.
[2] Doggrell S.  Do peroxisome proliferation receptor-gamma antagonists have clinical potential as combined antiobesity and antidiabetic drugs Expert Opin Investig Drugs. 2003 Apr;12(4):713-6.