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GSK0660

CAS No. : 1014691-61-2

产品活性：GSK0660 is a potent antagonist of PPARβ and PPARδ, with IC₅₀s of 155 nM for both isoforms.

研究领域：Cell Cycle/DNA Damage  |  Vitamin D Related/Nuclear Receptor

作用靶点：PPAR

In Vitro: GSK0660 is a potent antagonist of PPARβ and PPARδ, with IC₅₀s of both 155 nM, and is nearly inactive on PPARα and PPARγ with IC₅₀s of both >10 μM. GSK0660 antagonizes 100% of the activity of PPARβ/δ with a pIC₅₀ of 6.8. GSK0660 (100 nM) reduces CPT1a (a PPARβ/δ target gene) expression below the basal vehicle-treated level by approximately 50%, but shows no effect on PDK4 expression, which is also a PPARβ/δ target gene in skeletal muscle cells. GSK0660 (0.5 μM) reduces the levels of AMPK and eNOS phosphorylation, and BMP-2, Runx-2 mRNA expression in MC3T3-E1 cells. GSK0660 (0.1 and 0.5 μM) reverses the bezafibrate-induced enchancement of ALP activity on d 7 in MC3T3-E1 cells. GSK0660 (1 μM) markedly blocks GW501516-mediated attenuation of glutamate release, and the effect of GW501516 on ROS generation in BV-2 cells stimulated with LPS. Furthermore, GSK0660 significantly reduces inhibitory effect of GW501516 on the LPS-induced expression of gp91phox mRNA in BV-2 cells.

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