eprotirome (BioDeep_00000605757)
代谢物信息卡片
化学式: C18H17Br2NO5 (484.94733920000004)
中文名称: 伊罗替罗
谱图信息:
最多检出来源 () 0%
分子结构信息
SMILES: CC(C)C1=C(C=CC(=C1)OC2=C(C=C(C=C2Br)NC(=O)CC(=O)O)Br)O
InChI: InChI=1S/C18H17Br2NO5/c1-9(2)12-7-11(3-4-15(12)22)26-18-13(19)5-10(6-14(18)20)21-16(23)8-17(24)25/h3-7,9,22H,8H2,1-2H3,(H,21,23)(H,24,25)
描述信息
C78276 - Agent Affecting Digestive System or Metabolism > C29703 - Antilipidemic Agent
Eprotirome (KB2115) is a liver-selective thyroid hormone receptor (TR) agonist. KB2115 has modestly higher affinity for TRβ than for TRα. Eprotirome reduces low-density lipoprotein (LDL) cholesterol concentrations. Eprotirome can be used for dyslipidemias and obesity research[1][2].
同义名列表
数据库引用编号
6 个数据库交叉引用编号
- PubChem: 10299876
- Metlin: METLIN64713
- DrugBank: DB05035
- ChEMBL: CHEMBL2035874
- CAS: 355129-15-6
- medchemexpress: HY-10473
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。
文献列表
- Riccardo Zucchi. Thyroid Hormone Analogues: An Update.
Thyroid : official journal of the American Thyroid Association.
2020 08; 30(8):1099-1105. doi:
10.1089/thy.2020.0071
. [PMID: 32098589] - Rosalba Senese, Federica Cioffi, Giuseppe Petito, Fernando Goglia, Antonia Lanni. Thyroid hormone metabolites and analogues.
Endocrine.
2019 10; 66(1):105-114. doi:
10.1007/s12020-019-02025-5
. [PMID: 31359245] - Simone Kersseboom, Anja L M van Gucht, Alies van Mullem, Giulia Brigante, Stefania Farina, Bo Carlsson, Joanne M Donkers, Stan F J van de Graaf, Robin P Peeters, Theo J Visser. Role of the Bile Acid Transporter SLC10A1 in Liver Targeting of the Lipid-Lowering Thyroid Hormone Analog Eprotirome.
Endocrinology.
2017 10; 158(10):3307-3318. doi:
10.1210/en.2017-00433
. [PMID: 28938430] - Marta Szydlowska, Monica Pibiri, Andrea Perra, Elisabetta Puliga, Sandra Mattu, Giovanna M Ledda-Columbano, Amedeo Columbano, Vera P Leoni. The Thyromimetic KB2115 (Eprotirome) Induces Rat Hepatocyte Proliferation.
Gene expression.
2017 Jul; 17(3):207-218. doi:
10.3727/105221617x695438
. [PMID: 28409553] - Bo Angelin, Jens D Kristensen, Mats Eriksson, Bo Carlsson, Irwin Klein, Anders G Olsson, E Chester Ridgway, Paul W Ladenson. Reductions in serum levels of LDL cholesterol, apolipoprotein B, triglycerides and lipoprotein(a) in hypercholesterolaemic patients treated with the liver-selective thyroid hormone receptor agonist eprotirome.
Journal of internal medicine.
2015 Mar; 277(3):331-342. doi:
10.1111/joim.12261
. [PMID: 24754313] - Ylva Bonde, Olof Breuer, Dieter Lütjohann, Stefan Sjöberg, Bo Angelin, Mats Rudling. Thyroid hormone reduces PCSK9 and stimulates bile acid synthesis in humans.
Journal of lipid research.
2014 Nov; 55(11):2408-15. doi:
10.1194/jlr.m051664
. [PMID: 25172631] - Barbara Sjouke, Gisle Langslet, Richard Ceska, Stephen J Nicholls, Steven E Nissen, Maria Öhlander, Paul W Ladenson, Anders G Olsson, G Kees Hovingh, John J P Kastelein. Eprotirome in patients with familial hypercholesterolaemia (the AKKA trial): a randomised, double-blind, placebo-controlled phase 3 study.
The lancet. Diabetes & endocrinology.
2014 Jun; 2(6):455-63. doi:
10.1016/s2213-8587(14)70006-3
. [PMID: 24731671] - Martha J Kelly, Sherrie Pietranico-Cole, J Douglas Larigan, Nancy-Ellen Haynes, Charles H Reynolds, Nathan Scott, John Vermeulen, Mark Dvorozniak, Karin Conde-Knape, Kuo-Sen Huang, Sung-Sau So, Kshitij Thakkar, Yimin Qian, Bruce Banner, Frank Mennona, Sara Danzi, Irwin Klein, Rebecca Taub, Jefferson Tilley. Discovery of 2-[3,5-dichloro-4-(5-isopropyl-6-oxo-1,6-dihydropyridazin-3-yloxy)phenyl]-3,5-dioxo-2,3,4,5-tetrahydro[1,2,4]triazine-6-carbonitrile (MGL-3196), a Highly Selective Thyroid Hormone Receptor β agonist in clinical trials for the treatment of dyslipidemia.
Journal of medicinal chemistry.
2014 May; 57(10):3912-23. doi:
10.1021/jm4019299
. [PMID: 24712661] - Daniel F Vatner, Dirk Weismann, Sara A Beddow, Naoki Kumashiro, Derek M Erion, Xiao-Hui Liao, Gary J Grover, Paul Webb, Kevin J Phillips, Roy E Weiss, Jonathan S Bogan, John Baxter, Gerald I Shulman, Varman T Samuel. Thyroid hormone receptor-β agonists prevent hepatic steatosis in fat-fed rats but impair insulin sensitivity via discrete pathways.
American journal of physiology. Endocrinology and metabolism.
2013 Jul; 305(1):E89-100. doi:
10.1152/ajpendo.00573.2012
. [PMID: 23651850] - Jean Z Lin, Alexandro J Martagón, Willa A Hsueh, John D Baxter, Jan-Åke Gustafsson, Paul Webb, Kevin J Phillips. Thyroid hormone receptor agonists reduce serum cholesterol independent of the LDL receptor.
Endocrinology.
2012 Dec; 153(12):6136-44. doi:
10.1210/en.2011-2081
. [PMID: 23087171] - Hiroaki Shiohara, Tetsuya Nakamura, Norihiko Kikuchi, Tomonaga Ozawa, Ryuichi Nagano, Akane Matsuzawa, Hideki Ohnota, Takahide Miyamoto, Kazuo Ichikawa, Kiyoshi Hashizume. Discovery of novel indane derivatives as liver-selective thyroid hormone receptor β (TRβ) agonists for the treatment of dyslipidemia.
Bioorganic & medicinal chemistry.
2012 Jun; 20(11):3622-34. doi:
10.1016/j.bmc.2012.03.056
. [PMID: 22542282] - Klaus G Parhofer. Mipomersen: evidence-based review of its potential in the treatment of homozygous and severe heterozygous familial hypercholesterolemia.
Core evidence.
2012; 7(?):29-38. doi:
10.2147/ce.s25239
. [PMID: 22701100] - B Sjouke, D M Kusters, J J P Kastelein, G K Hovingh. Familial hypercholesterolemia: present and future management.
Current cardiology reports.
2011 Dec; 13(6):527-36. doi:
10.1007/s11886-011-0219-9
. [PMID: 21938413] - Klaus G Parhofer. Lipoprotein(a): medical treatment options for an elusive molecule.
Current pharmaceutical design.
2011; 17(9):871-6. doi:
10.2174/138161211795428777
. [PMID: 21476974] - Heiner K Berthold, Matthias Laudes, Wilhelm Krone, Ioanna Gouni-Berthold. Association between the interleukin-6 promoter polymorphism -174G/C and serum lipoprotein(a) concentrations in humans.
PloS one.
2011; 6(9):e24719. doi:
10.1371/journal.pone.0024719
. [PMID: 21935443] - Børge G Nordestgaard, M John Chapman, Kausik Ray, Jan Borén, Felicita Andreotti, Gerald F Watts, Henry Ginsberg, Pierre Amarenco, Alberico Catapano, Olivier S Descamps, Edward Fisher, Petri T Kovanen, Jan Albert Kuivenhoven, Philippe Lesnik, Luis Masana, Zeljko Reiner, Marja-Riitta Taskinen, Lale Tokgözoglu, Anne Tybjærg-Hansen. Lipoprotein(a) as a cardiovascular risk factor: current status.
European heart journal.
2010 Dec; 31(23):2844-53. doi:
10.1093/eurheartj/ehq386
. [PMID: 20965889] - Bo Angelin, Mats Rudling. Lipid lowering with thyroid hormone and thyromimetics.
Current opinion in lipidology.
2010 Dec; 21(6):499-506. doi:
10.1097/mol.0b013e3283402e9c
. [PMID: 20935564] - Federica Cioffi, Antonia Lanni, Fernando Goglia. Thyroid hormones, mitochondrial bioenergetics and lipid handling.
Current opinion in endocrinology, diabetes, and obesity.
2010 Oct; 17(5):402-7. doi:
10.1097/med.0b013e32833cf354
. [PMID: 20625286] - Paul Webb. Thyroid hormone receptor and lipid regulation.
Current opinion in investigational drugs (London, England : 2000).
2010 Oct; 11(10):1135-42. doi:
"
. [PMID: 20872316] - Anders G Olsson. Recent advances in preventing cardiovascular disorders by managing lipid levels.
F1000 medicine reports.
2010 Sep; 2(?):66. doi:
10.3410/m2-66
. [PMID: 21173859] - Nadeem Sarwar, Manjinder S Sandhu, Sally L Ricketts, Adam S Butterworth, Emanuele Di Angelantonio, S Matthijs Boekholdt, Willem Ouwehand, Hugh Watkins, Nilesh J Samani, Danish Saleheen, Debbie Lawlor, Muredach P Reilly, Aroon D Hingorani, Philippa J Talmud, John Danesh. Triglyceride-mediated pathways and coronary disease: collaborative analysis of 101 studies.
Lancet (London, England).
2010 May; 375(9726):1634-9. doi:
10.1016/s0140-6736(10)60545-4
. [PMID: 20452521] - Paul W Ladenson, Jens D Kristensen, E Chester Ridgway, Anders G Olsson, Bo Carlsson, Irwin Klein, John D Baxter, Bo Angelin. Use of the thyroid hormone analogue eprotirome in statin-treated dyslipidemia.
The New England journal of medicine.
2010 Mar; 362(10):906-16. doi:
10.1056/nejmoa0905633
. [PMID: 20220185] - Ivan Tancevski, Philipp Eller, Josef R Patsch, Andreas Ritsch. The resurgence of thyromimetics as lipid-modifying agents.
Current opinion in investigational drugs (London, England : 2000).
2009 Sep; 10(9):912-8. doi:
NULL
. [PMID: 19705333] - C Josseaume, Y Lorcy. [Thyroid hormone analogs: an important biological supply and new therapeutic possibilities].
Annales d'endocrinologie.
2008 Sep; 69 Suppl 1(?):S33-6. doi:
10.1016/s0003-4266(08)73966-0
. [PMID: 18954857] - Anders Berkenstam, Jens Kristensen, Karin Mellström, Bo Carlsson, Johan Malm, Stefan Rehnmark, Neeraj Garg, Carl Magnus Andersson, Mats Rudling, Folke Sjöberg, Bo Angelin, John D Baxter. The thyroid hormone mimetic compound KB2115 lowers plasma LDL cholesterol and stimulates bile acid synthesis without cardiac effects in humans.
Proceedings of the National Academy of Sciences of the United States of America.
2008 Jan; 105(2):663-7. doi:
10.1073/pnas.0705286104
. [PMID: 18160532]