您好,欢迎来到试剂信息网! [登录] [免费注册]
试剂信息网
位置:首页 > 产品库 > SR 202
立即咨询
咨询类型:
     
*姓名:
*电话:
*单位:
Email:
*留言内容:
请详细说明您的需求。
*验证码:
 
SR 202
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
SR 202图片
CAS NO:76541-72-5
规格:98%
分子量:358.65
包装与价格:
包装价格(元)
1mg电议
5mg电议

产品介绍
PPAR antagonist
CAS:76541-72-5
分子式:C11H17ClO7P2
分子量:358.65
纯度:98%
存储:Store at -20°C

Background:

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.


参考文献:
[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.