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CAS No.: 101574-65-6

GSK-4716 Catalog No. CSN22842

Synonyms: GSK 4716

GSK4716 is an agonist of ERRβ/γ with IC50 of 2 µM with similar potency as the protein ligand PGC-1α.

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技术信息

生物活性

描述Estrogen related receptors (ERRs) are orphan nuclear receptors that are closely related to estrogen receptors (ERR and ER). Thus far, three isoforms of ERRs (ERRR, ERR, and ERRγ) have been identified^[1]. Estrogen receptors are key receptors to maintain ovarian granulosa cell differentiation, follicle and oocyte growth and development, and ovulation function^[2]. GSK-4716 is a selective ERRβ/γ agonist^[3]. Treatment of differentiated C2C12 cells with GSK 4716 (relative to vehicle) over a 2 to 4 h time reveals a reproducible and robust increase in the immunoreactivity of the GRα-D isoform. It is observed that MAO-A mRNA expression is significantly increased by treatment. Furthermore, GSK4716 induces the expression of the mRNAs encoding peroxisome proliferator-activated receptor-γcoactivator 1α (PGC-1α) and PGC-1β (key regulator of many metabolic genes) identified as direct coactivators for the ERR family. It also induces the expression of PGC-1 and genes involved in fatty acid oxidation in concordance with the characterized role of ERRγ in cardiac metabolism. Treatment of primary mouse myotubes with GSK4716, GSK 4716, results in a concerted increase in the expression levels of Ppargc1a, Ppargc1b, and the Esrr genes. Furthermore, Cpt1b, Atp5b, and Idh3, in key mitochondrial pathways, are also induced by GSK4716. Additionally, GSK4716 increases citrate synthase activity and cytochrome c protein levels^[4].
参考文献

[1] Yongju Kim,et al. Efficient Discovery of Selective Small Molecule Agonists of Estrogen-Related Receptor γ using Combinatorial Approach. J Comb Chem. Sep-Oct 2009;11(5):928-37.
[2] Zi-Run Tang,et al. Estrogen-Receptor Expression and Function in Female Reproductive Disease, Cells. 2019 Sep 21;8(10):1123.
[3] 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.
[4] Rangwala SM, et al. Estrogen-related receptor gamma is a key regulator of muscle mitochondrial activity and oxidative capacity. J Biol Chem. 2010 Jul 16;285(29):22619-29.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.5419 mL
- 17.7093 mL
- 35.4187 mL
- 5 mM
- 0.7084 mL
- 3.5419 mL
- 7.0837 mL
- 10 mM
- 0.3542 mL
- 1.7709 mL
- 3.5419 mL

技术信息

CAS号

101574-65-6

储存条件

粉末: Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C17H18N2O2

运输

蓝冰

分子量

282.34

别名

GSK 4716

溶解度

DMSO	490.0 mg/mL (1735.5 mM)
Water	insoluble

动物实验配方

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