| Identification | Back Directory | [Name]
(4-CHLOROPHENYL)(DIMETHOXYPHOSPHINYL)METHYL PHOSPHORIC ACID DIMETHYL ESTER | [CAS]
76541-72-5 | [Synonyms]
SR 202
MIFOBATE
Clenicor
claniclor
SR-202 >=98% (HPLC), crystalline
Dimethyl (α-dimethoxyphosphinyl-p-chlorobenzyl) phosphate
DIMETHYL (ALPHA-DIMETHOXYPHOSPHINYL-P-CHLOROBENZYL) PHOSPHATE
[(4-Chlorophenyl)(dimethoxyphosphinyl)methyl]dimethyl=phosphate
Dimethyl (α-dimethoxyphosphinyl-p-chlorobenzyl) phosphate, Mifobate
phosphoricacid,(4-chlorophenyl)(dimethoxyphosphinyl)methyldimethylester
(4-CHLOROPHENYL)(DIMETHOXYPHOSPHINYL)METHYL PHOSPHORIC ACID DIMETHYL ESTER | [Molecular Formula]
C11H17ClO7P2 | [MDL Number]
MFCD01748280 | [MOL File]
76541-72-5.mol | [Molecular Weight]
358.65 |
| Questions And Answer | Back Directory | [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. |
| Chemical Properties | Back Directory | [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 |
| Hazard Information | Back Directory | [Uses]
Anti-atherosclerotic. | [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. |
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