SR 202 Chemical Properties

Boiling point:

436.6±45.0 °C(Predicted)

Density 

1.355±0.06 g/cm3(Predicted)

storage temp. 

Inert atmosphere,Store in freezer, under -20°C

solubility 

DMSO: 5 mg/mL

form 

crystalline

color 

white

Water Solubility 

Soluble to 100 mM in water

Safety Information

Safety Statements 

22-24/25

WGK Germany 

2

RTECS 

TB8817000

MSDS

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SR 202 Usage And Synthesis

Description

SR 202 is an effective and specific PPARγ antagonist that selectively inhibits the transcriptional activity of PPARγ induced by TZD (IC50=140 μM). Sr-202 does not affect basal or ligand stimulated transcriptional activity of PPARα, PPARβ, or FXR. It has anti-obesity and anti-diabetes effects.

Uses

Anti-atherosclerotic.

Uses

SR 202 is a noniodinated, potential lipid-altering agent and an inhibitor of the peripheral conversion of T4 to T3 associated with thyroid hormone metabolism.

Definition

ChEBI: Phosphoric acid [(4-chlorophenyl)-dimethoxyphosphorylmethyl] dimethyl ester is a trialkyl phosphate.

brand name

Clenicor (Symphar S.A.,Switzerland).

Biological Activity

Selective PPAR γ antagonist; antidiabetic and antiobesity agent. Attenuates troglitazone-induced PPAR γ transcriptional activity (IC 50 = 140 μ M) without affecting ligand-stimulated PPAR α , PPAR β or FXR transcriptional activity. Inhibits PPAR γ -dependent adipocyte differentiation and growth in vitro and in vivo . Improves insulin sensitivity in diabetic ob/ob mice and increases HDL levels in rats in vivo .

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]..

IC 50

140 μm for attenuation of troglitazone-induced peroxisome proliferator-activated receptor gamma (ppar) transcriptional activity [1]

storage

Desiccate at RT

References

[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.

SR 202(76541-72-5)Related Product Information

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