Varespladib (BioDeep_00000858936)
代谢物信息卡片
Varespladib
化学式: C21H20N2O5 (380.137215)
中文名称: 伐瑞拉迪
谱图信息:
最多检出来源 () 0%
分子结构信息
SMILES: CCC1=C(C2=C(N1CC3=CC=CC=C3)C=CC=C2OCC(=O)O)C(=O)C(=O)N
InChI: InChI=1S/C21H20N2O5/c1-2-14-19(20(26)21(22)27)18-15(9-6-10-16(18)28-12-17(24)25)23(14)11-13-7-4-3-5-8-13/h3-10H,2,11-12H2,1H3,(H2,22,27)(H,24,25)
描述信息
C78272 - Agent Affecting Nervous System > C241 - Analgesic Agent > C2198 - Nonnarcotic Analgesic
COVID info from clinicaltrial, clinicaltrials, clinical trial, clinical trials
Corona-virus
Coronavirus
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Varespladib (LY315920) is a potent and selective group IIA, secretory phospholipase A2 (sPLA2) inhibitor with an IC50 of 9 nM. Varespladib exhibits the significant inhibitory effect on sPLA2 activity in serum from various species including rat, rabbit, guinea pig and human with IC50s of 8.1 nM, 5.0 nM, 3.2 nM and 6.2 nM, respectively[1].
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
- ChEBI: CHEBI:189668
- KEGGdrug: D08107
- PubChem: 155815
- DrugBank: DB11909
- ChEMBL: CHEMBL148674
- CAS: 172732-68-2
- medchemexpress: HY-13402
分类词条
相关代谢途径
Reactome(0)
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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
- Ganesh H Sampat, Kashinath Hiremath, Jagadeesh Dodakallanavar, Vishal S Patil, Darasaguppe R Harish, Prakash Biradar, Rashmi K Mahadevamurthy, Manish Barvaliya, Subarna Roy. Unraveling snake venom phospholipase A2: an overview of its structure, pharmacology, and inhibitors.
Pharmacological reports : PR.
2023 Nov; ?(?):. doi:
10.1007/s43440-023-00543-8. [PMID: 37926795] - Rui Wang, Dan Gao, Fanglin Yu, Jiamin Han, Hai Yuan, Fengqi Hu. Phospholipase A2 inhibitor varespladib prevents wasp sting-induced nephrotoxicity in rats.
Toxicon : official journal of the International Society on Toxinology.
2022 Aug; 215(?):69-76. doi:
10.1016/j.toxicon.2022.06.007. [PMID: 35724947] - Rosimeire Silva-Carvalho, Matheus Z Gaspar, Luiz H B Quadros, Luís G G Lobo, Letícia M Rogério, Najla T S Santos, Maria C Zerbinatti, Cecília L Santarém, Elisangela O Silva, Juliana R Gerez, Nelson J Silva, Bruno Lomonte, Edward G Rowan, Rafael S Floriano. In vivo treatment with varespladib, a phospholipase A2 inhibitor, prevents the peripheral neurotoxicity and systemic disorders induced by Micrurus corallinus (coral snake) venom in rats.
Toxicology letters.
2022 Mar; 356(?):54-63. doi:
10.1016/j.toxlet.2021.11.003. [PMID: 34774704] - Varnavas D Mouchlis, Aaron Armando, Edward A Dennis. Substrate-Specific Inhibition Constants for Phospholipase A2 Acting on Unique Phospholipid Substrates in Mixed Micelles and Membranes Using Lipidomics.
Journal of medicinal chemistry.
2019 02; 62(4):1999-2007. doi:
10.1021/acs.jmedchem.8b01568. [PMID: 30615445] - Yiding Wang, Jing Zhang, Denghong Zhang, Huixiang Xiao, Shengwei Xiong, Chunhong Huang. Exploration of the Inhibitory Potential of Varespladib for Snakebite Envenomation.
Molecules (Basel, Switzerland).
2018 Feb; 23(2):. doi:
10.3390/molecules23020391. [PMID: 29439513] - Samuel Hernandez-Anzaldo, Vesna Brglez, Bianca Hemmeryckx, Dickson Leung, Janos G Filep, Jean E Vance, Dennis E Vance, Zamaneh Kassiri, Roger H Lijnen, Gérard Lambeau, Carlos Fernandez-Patron. Novel Role for Matrix Metalloproteinase 9 in Modulation of Cholesterol Metabolism.
Journal of the American Heart Association.
2016 09; 5(10):. doi:
10.1161/jaha.116.004228. [PMID: 27694328] - Samuel Hernandez-Anzaldo, Evan Berry, Vesna Brglez, Dickson Leung, Tae Jin Yun, Jun Seong Lee, Janos G Filep, Zamaneh Kassiri, Cheolho Cheong, Gérard Lambeau, Richard Lehner, Carlos Fernandez-Patron. Identification of a Novel Heart-Liver Axis: Matrix Metalloproteinase-2 Negatively Regulates Cardiac Secreted Phospholipase A2 to Modulate Lipid Metabolism and Inflammation in the Liver.
Journal of the American Heart Association.
2015 Nov; 4(11):. doi:
10.1161/jaha.115.002553. [PMID: 26567374] - Stephen J Nicholls, John J P Kastelein, Gregory G Schwartz, Dianna Bash, Robert S Rosenson, Matthew A Cavender, Danielle M Brennan, Wolfgang Koenig, J Wouter Jukema, Vijay Nambi, R Scott Wright, Venu Menon, A Michael Lincoff, Steven E Nissen. Varespladib and cardiovascular events in patients with an acute coronary syndrome: the VISTA-16 randomized clinical trial.
JAMA.
2014 Jan; 311(3):252-62. doi:
10.1001/jama.2013.282836. [PMID: 24247616] - Eva Hurt-Camejo, Thomas Gautier, Birgitta Rosengren, Arne Dikkers, Margareta Behrendt, David S Grass, Daniel J Rader, Uwe J F Tietge. Expression of type IIA secretory phospholipase A2 inhibits cholesteryl ester transfer protein activity in transgenic mice.
Arteriosclerosis, thrombosis, and vascular biology.
2013 Dec; 33(12):2707-14. doi:
10.1161/atvbaha.113.301410. [PMID: 24115030] - Robert S Rosenson. After FRANCIS: next steps in the clinical evaluation of varespladib methyl.
Future cardiology.
2011 Jan; 7(1):11-8. doi:
10.2217/fca.10.118. [PMID: 21174506] - Robert S Rosenson, Michael H Gelb. Secretory phospholipase A2: a multifaceted family of proatherogenic enzymes.
Current cardiology reports.
2009 Nov; 11(6):445-51. doi:
10.1007/s11886-009-0064-2. [PMID: 19863869] - Hector M Garcia-Garcia, Patrick W Serruys. Phospholipase A2 inhibitors.
Current opinion in lipidology.
2009 Aug; 20(4):327-32. doi:
10.1097/mol.0b013e32832dd4c7. [PMID: 19550325] - Zory Shaposhnik, Xuping Wang, Joaquim Trias, Heather Fraser, Aldons J Lusis. The synergistic inhibition of atherogenesis in apoE-/- mice between pravastatin and the sPLA2 inhibitor varespladib (A-002).
Journal of lipid research.
2009 Apr; 50(4):623-9. doi:
10.1194/jlr.m800361-jlr200. [PMID: 19029066] - Jose O Leite, Ushma Vaishnav, Michael Puglisi, Heather Fraser, Joaquim Trias, Maria Luz Fernandez. A-002 (Varespladib), a phospholipase A2 inhibitor, reduces atherosclerosis in guinea pigs.
BMC cardiovascular disorders.
2009 Feb; 9(?):7. doi:
10.1186/1471-2261-9-7. [PMID: 19222850] - Heather Fraser, Colin Hislop, Robert M Christie, Heather L Rick, Charles A Reidy, Michael L Chouinard, Patrick I Eacho, Kenneth E Gould, Joaquim Trias. Varespladib (A-002), a secretory phospholipase A2 inhibitor, reduces atherosclerosis and aneurysm formation in ApoE-/- mice.
Journal of cardiovascular pharmacology.
2009 Jan; 53(1):60-5. doi:
10.1097/fjc.0b013e318195bfbc. [PMID: 19129734] - Bernhardt G Zeiher, Jay Steingrub, Pierre-Francois Laterre, Alex Dmitrienko, Yonetaka Fukiishi, Edward Abraham. LY315920NA/S-5920, a selective inhibitor of group IIA secretory phospholipase A2, fails to improve clinical outcome for patients with severe sepsis.
Critical care medicine.
2005 Aug; 33(8):1741-8. doi:
10.1097/01.ccm.0000171540.54520.69. [PMID: 16096451] - Yasuhiko Tomita, Kenji Kuwabara, Shingo Furue, Kazushige Tanaka, Katsutoshi Yamada, Masahiko Ueno, Takashi Ono, Toshiyuki Maruyama, Tetsuo Ajiki, Hirohiko Onoyama, Masahiro Yamamoto, Yozo Hori. Effect of a selective inhibitor of secretory phospholipase A2, S-5920/LY315920Na, on experimental acute pancreatitis in rats.
Journal of pharmacological sciences.
2004 Oct; 96(2):144-54. doi:
10.1254/jphs.fp0040314. [PMID: 15467263] - Edward Abraham, Chris Naum, Venkata Bandi, Daniel Gervich, Stephen F Lowry, Richard Wunderink, Roland M Schein, William Macias, Simona Skerjanec, Alex Dmitrienko, Nagy Farid, S Thomas Forgue, Frank Jiang. Efficacy and safety of LY315920Na/S-5920, a selective inhibitor of 14-kDa group IIA secretory phospholipase A2, in patients with suspected sepsis and organ failure.
Critical care medicine.
2003 Mar; 31(3):718-28. doi:
10.1097/01.ccm.0000053648.42884.89. [PMID: 12626975] - K Koike, Y Yamamoto, Y Hori, T Ono. Group IIA phospholipase A2 mediates lung injury in intestinal ischemia-reperfusion.
Annals of surgery.
2000 Jul; 232(1):90-7. doi:
10.1097/00000658-200007000-00013. [PMID: 10862200] - S Furue, K Kuwabara, K Mikawa, K Nishina, M Shiga, N Maekawa, M Ueno, Y Chikazawa, T Ono, Y Hori, A Matsukawa, M Yoshinaga, H Obara. Crucial role of group IIA phospholipase A(2) in oleic acid-induced acute lung injury in rabbits.
American journal of respiratory and critical care medicine.
1999 Oct; 160(4):1292-302. doi:
10.1164/ajrccm.160.4.9812042. [PMID: 10508821] - T Yoshikawa, S Naruse, M Kitagawa, H Ishiguro, Y Nakae, T Ono, T Hayakawa. Effect of a new inhibitor of type II phospholipase A2 on experimental acute pancreatitis in rats.
Pancreas.
1999 Aug; 19(2):193-8. doi:
10.1097/00006676-199908000-00013. [PMID: 10438167] - D W Snyder, N J Bach, R D Dillard, S E Draheim, D G Carlson, N Fox, N W Roehm, C T Armstrong, C H Chang, L W Hartley, L M Johnson, C R Roman, A C Smith, M Song, J H Fleisch. Pharmacology of LY315920/S-5920, [[3-(aminooxoacetyl)-2-ethyl-1- (phenylmethyl)-1H-indol-4-yl]oxy] acetate, a potent and selective secretory phospholipase A2 inhibitor: A new class of anti-inflammatory drugs, SPI.
The Journal of pharmacology and experimental therapeutics.
1999 Mar; 288(3):1117-24. doi:
NULL. [PMID: 10027849]