产品描述: GSK4716 is an ERRβ/γ agonist (IC50 = 2 μM) that can activate the receptor with similar potency as the protein ligand |
靶点:
Estrogen Receptor/ERR;EstrogenReceptor/ERR |
细胞实验:
Mouse myoblasts were isolated as described previously.?Human ERRγ-IRES green fluorescent protein adenovirus was generated by Welgen.?Following a 48-h differentiation period, myotubes were transduced with green fluorescent protein or ERRγ adenovirus for 48 h. The titers to achieve low and high levels of ERRγ expression were 1* 10^8 and 5*10^8 virus particles/ml, respectively.?GSK4716 was synthesized as described previously and dissolved in DMSO for cell culture experiments.?Cells treated with a corresponding volume of DMSO were used as controls |
参考文献:
1.Wang L , Zuercher W J , Consler T G , et al. X-ray Crystal Structures of the Estrogen-related Receptor-? Ligand Binding Domain in Three Functional States Reveal the Molecular Basis of Small Molecule Regulation[J]. Journal of Biological Chemistry, 2006, 281(49):37773-37781. 2.Wang SC, et al. An ERRbeta/gamma agonist modulates GRalpha expression, and glucocorticoid responsive gene expression in skeletal muscle cells. Mol Cell Endocrinol. 2010 Feb 5;315(1-2):146-52. 3.Rangwala S M , Wang X , Calvo J A , et al. Estrogen-related Receptor ? Is a Key Regulator of Muscle Mitochondrial Activity and Oxidative Capacity[J]. Journal of Biological Chemistry, 2010, 285(29):22619-22629. |
溶解性:
DMSO:100 mg/mL (354.18 mM) |
保存条件:
2-8℃ |
配置溶液浓度参考:
|
1mg |
5mg |
10mg |
1 mM |
3.542 ml |
17.709 ml |
35.418 ml |
5 mM |
0.708 ml |
3.542 ml |
7.084 ml |
10 mM |
0.354 ml |
1.771 ml |
3.542 ml |
50 mM |
0.071 ml |
0.354 ml |
0.708 ml |
|
注意: |
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