T0070907 是一种有效且特异性的 PPARγ 抑制剂，Ki值为1 nM，其选择性比 PPARα 和 PPARδ 高 800 倍以上。

T0070907(IC50=1 nM) , an effective and specific PPARγ inhibitor, with the >800-fold selectivity over PPARα and PPARδ.

T0070907 can attenuate the beneficial effects of lipopolysaccharide pretreatment, such as significantly improving renal insufficiency, reducing hepatocyte damage and circulatory failure, and reducing plasma interleukin-1 elevation caused by severe endotoxemia.

Ligand Binding Assay: To determine the binding affinity of T0070907 to the PPARs, scintillation proximity assay (SPA) is performed with the following modifications. A 90-μl reaction contains SPA buffer (10 mm KH2PO4, 10 mm KH2PO4, 2 mm EDTA, 50 mm NaCl, 1 mm dithiothreitol, 2 mmCHAPS, 10% (v/v) glycerol, pH 7.1), 50 ng of GST-PPARγ (or 150 ng of GST-PPARα, GST-PPARδ), 5 nm 3H-labeled radioligands, and 5 μl of T0070907 in Me2SO. After incubation for 1 h at room temperature, 10 μl of polylysine-coated SPA beads (at 20 mg/ml in SPA buffer) are added, and the mixtureis incubated for 1 h before reading in Packard Topcount. [3H]Rosiglitazone is used for PPARγ, and [3H]GW2433 is used for PPARα and PPARδ.

MTS assay(Only for Reference)

313516-66-4

C12H8ClN3O3

277.66

DMSO:27.8 mg/mL (100 mM)
1eq. HCl:27.8 mg/mL (100 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years