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Products are for research use only. Not for human use. We do not sell to patients.
(T-0070907; T 0070907)
T0070907 Chemical Structure
|Product name: T0070907|
|Cat. No.: HY-13202|
T0070907 is a potent and selective PPARγ antagonist with IC50 of 1 nM; displays > 800-fold selectivity for PPARγ over PPARα and PPARδ.
IC50 Value: 1 nM
in vitro: 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: 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 [beta] caused by severe endotoxemia. T0070907 can attenuate all of these beneficial effects afforded by preconditioning with lipopolysaccharide.
|M.Wt||277.66||Storage||Please store the product under the recommended conditions in the Certificate of Analysis.|
|Solvent & Solubility||
DMSO 26 mg/mL; Water <1.1 mg/mL
|1 mg||5 mg||10 mg|
|1 mM||3.6015 mL||18.0076 mL||36.0153 mL|
|5 mM||0.7203 mL||3.6015 mL||7.2031 mL|
|10 mM||0.3602 mL||1.8008 mL||3.6015 mL|
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