SR 202 Property

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

Safety Statements 

22-24/25

WGK Germany 

2

RTECS 

TB8817000

Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P304+P340IF INHALED: Remove victim to fresh air and Keep at rest in a position comfortable for breathing.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

SR 202 Chemical Properties,Usage,Production

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.