产品信息
抗原名称
PPARγ
商品描述
T0070907是高活性PPARγ选择性拮抗剂，IC50为1 nM，比对PPARα和PPARδ的抑制性高800倍。
分子量
277.66
纯度
＞98%
可溶性
1eq. HCl : 27.8 mg/mL (100 mM)
DMSO : 27.8 mg/mL (100 mM)
DMSO : 27.8 mg/mL (100 mM)
外观
white
In vitro(体外研究)
T0070907 is a potent and selective PPARγ antagonist. With an apparent binding affinity (concentration at 50% inhibition of rosiglitazone binding or IC50) of 1 nM, T0070907 covalently modifies PPARγ on cysteine 313 in helix 3 of human PPARγ2. T0070907 blocks PPARγ function in both cell-based reporter gene and adipocyte differentiation assays. Consistent with its role as an antagonist of PPARγ, T0070907 blocks agonist-induced recruitment of coactivator-derived peptides to PPARγ in a homogeneous time-resolved fluorescence-based assay and promotes recruitment of the transcriptional corepressor NCoR to PPARγ in both glutathione S-transferase pull-down assays and a PPARγ/retinoid X receptor (RXR) α-dependent gel shift assay. Studies with mutant receptors suggest that T0070907 modulates the interaction of PPARγ with these cofactor proteins by affecting the conformation of helix 12 of the PPARγ ligand-binding domain. Interestingly, whereas the T0070907-induced NCoR recruitment to PPARγ/RXRα heterodimer can be almost completely reversed by the simultaneous treatment with RXRα agonist LGD1069, T0070907 treatment has only modest effects on LGD1069-induced coactivator recruitment to the PPARγ/RXRα heterodimer. T0070907 treatment inhibits proliferation, invasion and migration but does not significantly affect apoptosis. Molecular inhibition using a dominant negative (Δ462) receptor yields similar results. T007 also mediates a dose-dependent decrease in phosphorylation of PPARγ, and its ability to bind to DNA, and may directly affect mitogen-activated protein kinase signaling.
In vivo(体内研究)
Lipopolysaccharide preconditioning significantly attenuates the development of renal dysfunction, hepatocellular injury, and circulatory failure as well as the increase in the plasma levels of interleukin-1 caused by severe endotoxemia. T0070907 can attenuate all of these beneficial effects afforded by preconditioning with lipopolysaccharide
背景
别名
T-0070907; T 0070907
分子式
C12H8ClN3O3
CAS号
313516-66-4
制备和贮存
保存方式
Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.
参考图片
本文来自投稿，不代表本人立场，如若转载，请注明出处：http://www.iamyjet.com/article/20302.html