76541-72-5 Usage
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
Different sources of media describe the Uses of 76541-72-5 differently. You can refer to the following data:
1. Anti-atherosclerotic.
2. 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.
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]
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.
Check Digit Verification of cas no
The CAS Registry Mumber 76541-72-5 includes 8 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 5 digits, 7,6,5,4 and 1 respectively; the second part has 2 digits, 7 and 2 respectively.
Calculate Digit Verification of CAS Registry Number 76541-72:
(7*7)+(6*6)+(5*5)+(4*4)+(3*1)+(2*7)+(1*2)=145
145 % 10 = 5
So 76541-72-5 is a valid CAS Registry Number.
InChI:InChI=1/C11H17ClO7P2/c1-15-20(13,16-2)11(19-21(14,17-3)18-4)9-5-7-10(12)8-6-9/h5-8,11H,1-4H3
76541-72-5Relevant articles and documents
gem-Diphosphonate and gem-phosphonate-phosphate compounds with specific high density lipoprotein inducing activity
Nguyen,Niesor,Bentzen
, p. 1426 - 1433 (2007/10/02)
New diphosphonate compounds and related derivatives were synthesized and investigated for their activity in specifically inducing plasma high density lipoproteins (HDL) and high density lipoprotein cholesterol (HDL-C) in normal rats. The screening of nume
Novel Synthetic Aspects of the Phosphonate-Phosphate-Rearrangement. II. Synthesis of Enolphosphates from 1-Oxoalkanphosphonates and Sulfur-Ylides
Hammerschmidt, Friedrich,Zbiral, Erich
, p. 1015 - 1024 (2007/10/02)
Acylphosphonates 1 react with Sulfur-ylides 2 to give enolphosphates 3 and phosphonophosphates 4.The product ratio of 3 and 4 is determined by the substituent R3.If R3 is not electronwithdrawing the phosphonophosphate 4 is the sole reaction product. - Keywords: Acylphosphonates, behaviour towards S-ylides; Rearrangement of α-hydroxyphosphonates
