产品描述: | DY131 (GSK 9089) is a potent and selective ERRγ and ERRβ agonist. DY131displays inactive against ERRα, ERα and ERβ[1][2]. DY131 also inhibits Smo signaling |
靶点: |
ERRγ;ERRβ;EstrogenReceptor/ERR; Estrogen/progestogenReceptor; Smo |
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)[5] Dosage: 5 μg/kg Administration: Subcutaneous injection; every second day; for 12 days Result: Increased P450scc, StAR and HMGCR while decreased HSL expressions. |
参考文献: |
1. Yu S, et al. ERRgamma suppresses cell proliferation and tumor growth of androgen-sensitive and androgen-insensitive prostate cancer cells and its implication as a therapeutic target for prostate cancer. Cancer Res. 2007;67(10):4904-14. 2. Donna D. Yu, Barry Marc Forman. Identification of an agonist ligand for estrogen-related receptors ERRβ/γ. Bioorganic & Medicinal Chemistry Letters. 2005,15(5): 1311-1313. 3. Wang Y, et al. Selective identification of hedgehog pathway antagonists by direct analysis of smoothened ciliary translocation . ACS Chem Biol. 2012,15;7(6):1040-8. 4. Yamamoto T, et al. Estrogen-related receptor-γ regulates estrogen receptor-α responsiveness in uterine endometrial cancer. Int J Gynecol Cancer. 2012;22(9):1509-16. 5. A Pacwa, et al. Interplay between estrogen-related receptors and steroidogenesis-controlling molecules in adrenals. In vivo and in vitro study. Acta Histochem. 2018 Jul;120(5):456-467. |
溶解性: |
Soluble in DMSO |
保存条件: |
-20℃ |
配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
1 mM |
3.212 ml |
16.058 ml |
32.115 ml |
5 mM |
0.642 ml |
3.212 ml |
6.423 ml |
10 mM |
0.321 ml |
1.606 ml |
3.212 ml |
50 mM |
0.064 ml |
0.321 ml |
0.642 ml |
|
注意: |
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