产品
编 号:F536005
分子式:C18H21N3O2
分子量:311.38
产品类型
结构图
CAS No: 95167-41-2
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产品详情
生物活性:
DY131 (GSK 9089) is a potent and selective ERRγ and ERRβ agonist. DY131displays inactive against ERRα, ERα and ERβ. DY131 also inhibits Smo signaling.
体内研究:
DY131 (5 μg/kg; subcutaneous injection; every second day; for 12 days) treatment increases P450 side-chain cleavage (P450scc), StAR and HMGCoA reductase (HMGCR) while decreases hormone sensitive lipase (HSL) expressions.Animal Model:Mature male mice (C57BL/6) (8-10 week-old; ~24.3 g)
Dosage:5 μg/kg
Administration:Subcutaneous injection; every second day; for 12 days
Result:Increased P450scc, StAR and HMGCR while decreased HSL expressions.
体外研究:
DY131 (0.1-30 μM; 5 days) treatment suppresses cell proliferation and reduces BrdUrd-positive cells in both LNCaP-ERRγ and LNCaP cells in a dose-dependent manner, with higher suppression in LNCaP-ERRγ clone.DY131inhibits Shh induced accumulation of Smo::EGFP with an IC50 of 0.8 μM. DY131 suppresses SAG (100 nM) induced accumulation of Smo::EGFP in the primary cilium and Gli transcription activity with an IC50 of ~2 μM.DY131 dramatically decreases phosphorylated histone H3 (pH3) marked proliferation of CGNPs induced by Shh. A selective ERRγ agonist, DY131, inhibits the growth of the ERα-positive endometrial cancer cells but promoted that of the ERα-negative cancer cells.