GSK-4716-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEGSK-4716Cat. No.: HY-33353CAS No.: 101574-65-6分式: CHNO分量: 282.34作靶点: Estrogen Receptor/ERR作通路: Others储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 100 mg/mL (354.18 mM)* means soluble, bu

2、t saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 3.5418 mL 17.7091 mL 35.4183 mL5 mM 0.7084 mL 3.5418 mL 7.0837 mL10 mM 0.3542 mL 1.7709 mL 3.5418 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。体内实验请根据您的实验动物和给药式选择适当的溶解案，配制前请先配制澄的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的作液，建议您现现配，当天使；澄的储备液

3、可以根据储存条件，适当保存；以下溶剂前的百分指该溶剂在您配制终溶液中的体积占)：1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (8.85 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (8.85 mM); Clear solution3. 请依序添加每种溶剂： 10% DMSO 90% corn oil1/2 Master of Small Molecu

4、les 您边的抑制剂师www.MedChemESolubility: 2.5 mg/mL (8.85 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 GSK-4716种选择性 ERR/ 激动剂。IC50 & Target ERR/ 1体外研究 Treatment of differentiated C2C12 cells with the ERR/ agonist (relative to vehicle) over a 2 to 4 h timeperiod reveals a reproducible and robust increase in the

5、 immunoreactivity of the GR-D isoform. It isobserved that MAO-A mRNA expression is significantly increased by treatment with the ERR/ agonist,GSK4716. Furthermore, it is observed that GSK4716 induces the expression of the mRNAs encodingperoxisome proliferator-activated receptor-coactivator 1 (PGC-1)

6、 and PGC-1 (key regulator of manymetabolic genes) identified as direct coactivators for the ERR family. GSK4716 induces the expression ofPGC-1 and genes involved in fatty acid oxidation in concordance with the characterized role of ERR incardiac metabolism 1. Treatment of primary mouse myotubes with

7、 GSK4716, an ERR/ agonist, results ina concerted increase in the expression levels of Ppargc1a, Ppargc1b, and the Esrr genes.Furthermore,Cpt1b, Atp5b, and Idh3, genes in key mitochondrial pathways, are also induced by GSK4716.Additionally, GSK4716 increases citrate synthase activity and cytochrome c

8、 protein levels 2.PROTOCOLCell Assay 1 Proliferating mouse C2C12 myoblast are cultured and maintained in DMEM supplemented with 10% heat-inactivated serum supreme. Differentiation of myoblasts into post-mitotic, multi-nucleated myotubes areinduced by mitogen withdrawal (DMEM supplemented with 2% hor

9、se serum) for 4 days. C2C12 myotubesare treated with either vehicle (DMSO) or ERR/ agonist GSK4716 for 1 day and RNA collected andprocessed 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Wang SC, et al. An ERRbeta/gamma agonist modulates

10、 GRalpha expression, and glucocorticoid responsive gene expression in skeletalmuscle cells. Mol Cell Endocrinol. 2010 Feb 5;315(1-2):146-52.2. Rangwala SM, et al. Estrogen-related receptor gamma is a key regulator of muscle mitochondrial activity and oxidative capacity. J BiolChem. 2010 Jul 16;285(29):22619-29.McePdfHeightCaution: Product has not been fully val