GSK0660 是 PPARβ/δ 的拮抗剂和反向激动剂，IC50均为155 nM。

GSK0660 is an antagonist and inverse agonist of PPARβ/δ.

Human astrocytoma cells, 1321N1, are grown to stably express rat P2X7, human P2X4, P2X2a, P2X2/3, P2X1, P2Y1?and P2Y2 recombinant receptors. Agonist, BzATP, 2,3-O-(4-ben-zoylbenzoyl)-ATP or ATP-induced changes in intracellular Ca2+?concentrations are assessed in all of the cell lines using the Ca2+?chelating dye, Fluo-4, in conjunction with a Fluorometric Imaging Plate Reader. The cells are plated out the day before the experiment onto poly-D-lysine-coated black 96 well plates. After the agonist addition, changes in intracellular Ca2+ concentrations are recorded, per second, for 3 min. Ligands are tested at 11 half-log concentrations from 10-10 to 10-4 M. BzATP or ATP concentrations corresponds to the EC70?values for each receptor to enable comparison of antagonist potencies across the multiple P2 receptor subtypes. A 438079 is added to the cell plate and ?uorescence data are collected for 3 min before the addition of agonist, subsequently, data are then collected for another 2 min. The pEC50 or pIC50 values are derived from a single curve ?t.

1014691-61-2

C19H18N2O5S2

418.48

Ethanol:4.18 mg/mL (10 mM)
DMSO:41.85 mg/mL (100 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years