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FXR agonist 4
MCE 国际站：FXR agonist 4
产品活性：FXR agonist 4 (compound 10a) 是法尼酯 X 受体 (FXR) 激动剂，EC50 值为 1.05 μM。FXR agonist 4 有效改善 DIO 小鼠高脂血症、肝脏脂肪变性、胰岛素抵抗和肝脏炎症。FXR agonist 4 可用于非酒精性脂肪性肝病 (NAFLD) 的研究。
研究领域：Metabolic Enzyme/Protease
作用靶点：FXR
In Vitro: FXR agonist 4 (10 nM-10 μM) shows FXR agonistic activity with an EC50 value of 1.05 μM in HEK293T cells.
FXR agonist 4 (1 nM-10 μM) dose-dependently increarses steroid receptor coactivator (SRC)-2 recruitment with an EC50 value of 1.04 μM.
FXR agonist 4 (0.1 nM-10 μM) activates FXR in cells with fatty accumulation.
FXR agonist 4 (10-50 μM; 48 h) is not toxic to HepG2 cells.
In Vivo: FXR agonist 4 (100 mg/kg; oral administration, once) improves hyperlipidemia, hepatic steatosis, insulin resistance and hepatic inflammation in DIO mice.
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文献和实验Characterization of Nuclear Receptor Ligands by Multiplexed Peptide Interactions
, although described for nuclear receptors, may also be applied to other types of molecular interactions. Keywords: Microsphere; flow cytometry; nuclear receptor; coactivator; corepressor; cofactor; agonist; antagonist; ligand; ligand binding
: Birkh?user, 1994 [４5] Erlich H. PCR Technology: principles and applications for DNA amplification. New York, Stockton, 1989 [４6] 黄培堂, 俞炜源，等. PCR技术操作和应用指南. 北京: 科学出版社, 1990 [４7] 林万明. PCR技术操作和应用指南. 北京: 人民军医出版社, 1995 [４8] Brossas JY, Barreau E
19734881. ^ Wang XJ, Reyes JL, Chua NH, Gaasterland T (2004). "Prediction and identification of Arabidopsis thaliana microRNAs and their mRNA targets". Genome Biol. 5 (9): R65. doi:10.1186/gb-2004-5-9-r65. PMC 522872. PMID 15345049. http://genomebiology
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