Elafibranor (BioDeep_00000837657)
代谢物信息卡片
Elafibranor
化学式: C22H24O4S (384.1395)
中文名称:
谱图信息:
最多检出来源 () 0%
分子结构信息
SMILES: CC(C)(OC1=C(C)C=C(/C=C/C(C2=CC=C(SC)C=C2)=O)C=C1C)C(O)=O
InChI: InChI=1S/C22H24O4S/c1-14-12-16(13-15(2)20(14)26-22(3,4)21(24)25)6-11-19(23)17-7-9-18(27-5)10-8-17/h6-13H,1-5H3,(H,24,25)/b11-6+
描述信息
C78276 - Agent Affecting Digestive System or Metabolism > C29711 - Anti-diabetic Agent > C154291 - Peroxisome Proliferator-Activated Receptor Agonist
Elafibranor (GFT505) is a PPARα/δ agonist with EC50s of 45 and 175 nM, respectively.
同义名列表
2 个代谢物同义名
数据库引用编号
7 个数据库交叉引用编号
- KEGGdrug: D11208
- PubChem: 9864881
- DrugBank: DB05187
- ChEMBL: CHEMBL3707395
- CAS: 824932-88-9
- CAS: 923978-27-2
- medchemexpress: HY-16737
分类词条
相关代谢途径
Reactome(0)
BioCyc(0)
PlantCyc(0)
代谢反应
0 个相关的代谢反应过程信息。
Reactome(0)
BioCyc(0)
WikiPathways(0)
Plant Reactome(0)
INOH(0)
PlantCyc(0)
COVID-19 Disease Map(0)
PathBank(0)
PharmGKB(0)
0 个相关的物种来源信息
在这里通过桑基图来展示出与当前的这个代谢物在我们的BioDeep知识库中具有相关联信息的其他代谢物。在这里进行关联的信息来源主要有：
- PubMed: 来源于PubMed文献库中的文献信息，我们通过自然语言数据挖掘得到的在同一篇文献中被同时提及的相关代谢物列表，这个列表按照代谢物同时出现的文献数量降序排序，取前10个代谢物作为相关研究中关联性很高的代谢物集合展示在桑基图中。
- NCBI Taxonomy: 通过文献数据挖掘，得到的代谢物物种来源信息关联。这个关联信息同样按照出现的次数降序排序，取前10个代谢物作为高关联度的代谢物集合展示在桑吉图上。
- Chemical Taxonomy: 在物质分类上处于同一个分类集合中的其他代谢物
- Chemical Reaction: 在化学反应过程中，存在为当前代谢物相关联的生化反应过程中的反应底物或者反应产物的关联代谢物信息。
点击图上的相关代谢物的名称，可以跳转到相关代谢物的信息页面。
| 亚细胞结构定位 | 关联基因列表 |
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文献列表
- Cristina Zivko, Finja Witt, Andreas Koeberle, Gregor Fuhrmann, Paola Luciani. Formulating elafibranor and obeticholic acid with phospholipids decreases drug-induced association of SPARC to extracellular vesicles from LX-2 human hepatic stellate cells.
European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V.
2023 Jan; 182(?):32-40. doi:
10.1016/j.ejpb.2022.11.025. [PMID: 36470521] - Joost Boeckmans, Alexandra Gatzios, Anja Heymans, Matthias Rombaut, Vera Rogiers, Joery De Kock, Tamara Vanhaecke, Robim M Rodrigues. Transcriptomics Reveals Discordant Lipid Metabolism Effects between In Vitro Models Exposed to Elafibranor and Liver Samples of NAFLD Patients after Bariatric Surgery.
Cells.
2022 03; 11(5):. doi:
10.3390/cells11050893. [PMID: 35269515] - Kai Liu, Xing Zhao, Xue Qi, Dong-Liang Hou, Hao-Bin Li, Yu-Hao Gu, Qing-Long Xu. Design, synthesis, and biological evaluation of a novel dual peroxisome proliferator-activated receptor alpha/delta agonist for the treatment of diabetic kidney disease through anti-inflammatory mechanisms.
European journal of medicinal chemistry.
2021 Jun; 218(?):113388. doi:
10.1016/j.ejmech.2021.113388. [PMID: 33784603] - Joost Boeckmans, Alessandra Natale, Matthias Rombaut, Karolien Buyl, Brent Cami, Veerle De Boe, Anja Heymans, Vera Rogiers, Joery De Kock, Tamara Vanhaecke, Robim M Rodrigues. Human hepatic in vitro models reveal distinct anti-NASH potencies of PPAR agonists.
Cell biology and toxicology.
2021 04; 37(2):293-311. doi:
10.1007/s10565-020-09544-2. [PMID: 32613381] - Jingwen Zhou, Yidi Chen, Jun Yu, Tianci Li, Ziyu Lu, Yan Chen, Xiaolong Zhang, Fang Ye. The efficacy of novel metabolic targeted agents and natural plant drugs for nonalcoholic fatty liver disease treatment: A PRISMA-compliant network meta-analysis of randomized controlled trials.
Medicine.
2021 Mar; 100(12):e24884. doi:
10.1097/md.0000000000024884. [PMID: 33761646] - Anita M van den Hoek, Lars Verschuren, Martien P M Caspers, Nicole Worms, Aswin L Menke, Hans M G Princen. Beneficial effects of elafibranor on NASH in E3L.CETP mice and differences between mice and men.
Scientific reports.
2021 03; 11(1):5050. doi:
10.1038/s41598-021-83974-8. [PMID: 33658534] - May S Freag, Bumseok Namgung, Maria E Reyna Fernandez, Ermanno Gherardi, Shiladitya Sengupta, Hae Lin Jang. Human Nonalcoholic Steatohepatitis on a Chip.
Hepatology communications.
2021 02; 5(2):217-233. doi:
10.1002/hep4.1647. [PMID: 33553970] - Yu Yang, Yu Zhao, Wenzhen Li, Yuyao Wu, Xin Wang, Yijie Wang, Tingmei Liu, Tinghong Ye, Yongmei Xie, Zhiqiang Cheng, Jun He, Peng Bai, Yiwen Zhang, Liang Ouyang. Emerging targets and potential therapeutic agents in non-alcoholic fatty liver disease treatment.
European journal of medicinal chemistry.
2020 Jul; 197(?):112311. doi:
10.1016/j.ejmech.2020.112311. [PMID: 32339855] - F Anthony Romero, Christopher T Jones, Yingzi Xu, Martijn Fenaux, Randall L Halcomb. The Race to Bash NASH: Emerging Targets and Drug Development in a Complex Liver Disease.
Journal of medicinal chemistry.
2020 05; 63(10):5031-5073. doi:
10.1021/acs.jmedchem.9b01701. [PMID: 31930920] - Menso J Westerouen Van Meeteren, Joost P H Drenth, Eric T T L Tjwa. Elafibranor: a potential drug for the treatment of nonalcoholic steatohepatitis (NASH).
Expert opinion on investigational drugs.
2020 Feb; 29(2):117-123. doi:
10.1080/13543784.2020.1668375. [PMID: 31523999] - Emilia Gore, Emilia Bigaeva, Anouk Oldenburger, Yvette J M Jansen, Detlef Schuppan, Miriam Boersema, Jörg F Rippmann, Andre Broermann, Peter Olinga. Investigating fibrosis and inflammation in an ex vivo NASH murine model.
American journal of physiology. Gastrointestinal and liver physiology.
2020 02; 318(2):G336-G351. doi:
10.1152/ajpgi.00209.2019. [PMID: 31905025] - Maria Nicoline Baandrup Kristiansen, Sanne Skovgård Veidal, Christina Christoffersen, Michael Feigh, Niels Vrang, Jonathan David Roth, Mary Erickson, Luciano Adorini, Jacob Jelsing. Validity of biopsy-based drug effects in a diet-induced obese mouse model of biopsy-confirmed NASH.
BMC gastroenterology.
2019 Dec; 19(1):228. doi:
10.1186/s12876-019-1149-z. [PMID: 31883514] - Joost Boeckmans, Alessandra Natale, Matthias Rombaut, Karolien Buyl, Vera Rogiers, Joery De Kock, Tamara Vanhaecke, Robim M Rodrigues. Anti-NASH Drug Development Hitches a Lift on PPAR Agonism.
Cells.
2019 12; 9(1):. doi:
10.3390/cells9010037. [PMID: 31877771] - Jonathan D Roth, Sanne S Veidal, Louise K D Fensholdt, Kristoffer T G Rigbolt, Romeo Papazyan, Jens Christian Nielsen, Michael Feigh, Niels Vrang, Mark Young, Jacob Jelsing, Luciano Adorini, Henrik H Hansen. Combined obeticholic acid and elafibranor treatment promotes additive liver histological improvements in a diet-induced ob/ob mouse model of biopsy-confirmed NASH.
Scientific reports.
2019 06; 9(1):9046. doi:
10.1038/s41598-019-45178-z. [PMID: 31227742] - Joost Boeckmans, Karolien Buyl, Alessandra Natale, Valerie Vandenbempt, Steven Branson, Veerle De Boe, Vera Rogiers, Joery De Kock, Robim M Rodrigues, Tamara Vanhaecke. Elafibranor restricts lipogenic and inflammatory responses in a human skin stem cell-derived model of NASH.
Pharmacological research.
2019 06; 144(?):377-389. doi:
10.1016/j.phrs.2019.04.016. [PMID: 31028903] - Piero Pingitore, Kavitha Sasidharan, Matias Ekstrand, Sebastian Prill, Daniel Lindén, Stefano Romeo. Human Multilineage 3D Spheroids as a Model of Liver Steatosis and Fibrosis.
International journal of molecular sciences.
2019 Apr; 20(7):. doi:
10.3390/ijms20071629. [PMID: 30986904] - Tzu-Hao Li, Ying-Ying Yang, Chia-Chang Huang, Chih-Wei Liu, Hung-Cheng Tsai, Ming-Wei Lin, Chang-Youh Tsai, Shiang-Fen Huang, Ying-Wen Wang, Tzung-Yan Lee, Yi-Hsiang Huang, Ming-Chih Hou, Han-Chieh Lin. Elafibranor interrupts adipose dysfunction-mediated gut and liver injury in mice with alcoholic steatohepatitis.
Clinical science (London, England : 1979).
2019 02; 133(3):531-544. doi:
10.1042/cs20180873. [PMID: 30602573] - Hung-Cheng Tsai, Fu-Pang Chang, Tzu-Hao Li, Chih-Wei Liu, Chia-Chang Huang, Shiang-Fen Huang, Ying-Ying Yang, Kuei-Chuan Lee, Yun-Cheng Hsieh, Ying-Wen Wang, Tzung-Yan Lee, Yi-Hsiang Huang, Ming-Chih Hou, Han-Chieh Lin. Elafibranor Inhibits Chronic Kidney Disease Progression in NASH Mice.
BioMed research international.
2019; 2019(?):6740616. doi:
10.1155/2019/6740616. [PMID: 31321239] - Margherita Botta, Matteo Audano, Amirhossein Sahebkar, Cesare R Sirtori, Nico Mitro, Massimiliano Ruscica. PPAR Agonists and Metabolic Syndrome: An Established Role?.
International journal of molecular sciences.
2018 Apr; 19(4):. doi:
10.3390/ijms19041197. [PMID: 29662003] - Kirstine S Tølbøl, Maria Nb Kristiansen, Henrik H Hansen, Sanne S Veidal, Kristoffer Tg Rigbolt, Matthew P Gillum, Jacob Jelsing, Niels Vrang, Michael Feigh. Metabolic and hepatic effects of liraglutide, obeticholic acid and elafibranor in diet-induced obese mouse models of biopsy-confirmed nonalcoholic steatohepatitis.
World journal of gastroenterology.
2018 Jan; 24(2):179-194. doi:
10.3748/wjg.v24.i2.179. [PMID: 29375204] - Vlad Ratziu, Stephen A Harrison, Sven Francque, Pierre Bedossa, Philippe Lehert, Lawrence Serfaty, Manuel Romero-Gomez, Jérôme Boursier, Manal Abdelmalek, Steve Caldwell, Joost Drenth, Quentin M Anstee, Dean Hum, Remy Hanf, Alice Roudot, Sophie Megnien, Bart Staels, Arun Sanyal. Elafibranor, an Agonist of the Peroxisome Proliferator-Activated Receptor-α and -δ, Induces Resolution of Nonalcoholic Steatohepatitis Without Fibrosis Worsening.
Gastroenterology.
2016 05; 150(5):1147-1159.e5. doi:
10.1053/j.gastro.2016.01.038. [PMID: 26874076] - Rémy Hanf, Lesley J Millatt, Bertrand Cariou, Benoit Noel, Géraldine Rigou, Philippe Delataille, Valérie Daix, Dean W Hum, Bart Staels. The dual peroxisome proliferator-activated receptor alpha/delta agonist GFT505 exerts anti-diabetic effects in db/db mice without peroxisome proliferator-activated receptor gamma-associated adverse cardiac effects.
Diabetes & vascular disease research.
2014 Nov; 11(6):440-7. doi:
10.1177/1479164114548027. [PMID: 25212694] - Bertrand Cariou, Bart Staels. GFT505 for the treatment of nonalcoholic steatohepatitis and type 2 diabetes.
Expert opinion on investigational drugs.
2014 Oct; 23(10):1441-8. doi:
10.1517/13543784.2014.954034. [PMID: 25164277] - Amirhossein Sahebkar, Gerard T Chew, Gerald F Watts. New peroxisome proliferator-activated receptor agonists: potential treatments for atherogenic dyslipidemia and non-alcoholic fatty liver disease.
Expert opinion on pharmacotherapy.
2014 Mar; 15(4):493-503. doi:
10.1517/14656566.2014.876992. [PMID: 24428677] - Bart Staels, Anne Rubenstrunk, Benoit Noel, Géraldine Rigou, Philippe Delataille, Lesley J Millatt, Morgane Baron, Anthony Lucas, Anne Tailleux, Dean W Hum, Vlad Ratziu, Bertrand Cariou, Rémy Hanf. Hepatoprotective effects of the dual peroxisome proliferator-activated receptor alpha/delta agonist, GFT505, in rodent models of nonalcoholic fatty liver disease/nonalcoholic steatohepatitis.
Hepatology (Baltimore, Md.).
2013 Dec; 58(6):1941-52. doi:
10.1002/hep.26461. [PMID: 23703580] - Bertrand Cariou, Rémy Hanf, Stéphanie Lambert-Porcheron, Yassine Zaïr, Valérie Sauvinet, Benoit Noël, Laurent Flet, Hubert Vidal, Bart Staels, Martine Laville. Dual peroxisome proliferator-activated receptor α/δ agonist GFT505 improves hepatic and peripheral insulin sensitivity in abdominally obese subjects.
Diabetes care.
2013 Oct; 36(10):2923-30. doi:
10.2337/dc12-2012. [PMID: 23715754] - Sophie Colin, Olivier Briand, Véronique Touche, Kristiaan Wouters, Morgane Baron, François Pattou, Rémy Hanf, Anne Tailleux, Giulia Chinetti, Bart Staels, Sophie Lestavel. Activation of intestinal peroxisome proliferator-activated receptor-α increases high-density lipoprotein production.
European heart journal.
2013 Aug; 34(32):2566-74. doi:
10.1093/eurheartj/ehs227. [PMID: 22843443] - Bertrand Cariou, Yassine Zaïr, Bart Staels, Eric Bruckert. Effects of the new dual PPAR α/δ agonist GFT505 on lipid and glucose homeostasis in abdominally obese patients with combined dyslipidemia or impaired glucose metabolism.
Diabetes care.
2011 Sep; 34(9):2008-14. doi:
10.2337/dc11-0093. [PMID: 21816979]
