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Indomethacin

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Chemical Structure| 53-86-1 同义名 : Indometacin
CAS号 : 53-86-1
货号 : A502608
分子式 : C19H16ClNO4
纯度 : 97%
分子量 : 357.788
MDL号 : MFCD00057095
存储条件：

粉末 Keep in dark place,Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(293.47 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

无水乙醇: 12.5 mg/mL(34.94 mM)，配合低频超声助溶，注意：无水乙醇开封后，易挥发，也会吸收空气中的水分，导致溶解能力下降，请避免使用开封较久的乙醇
动物实验配方：

5% DMSO+30% PEG 300+5% Tween 80+water 2 mg/mL

生物活性
靶点

  • COX-2

    COX-2, IC50:14 μM

  • COX-1

    COX1, IC50:0.28 μM
描述 Indomethacin is a potent and nonselective inhibitor of COX1 and COX2, with IC50s of 18 nM and 26 nM for human COX-1 and COX-2, respectively, in CHO cells[3]. Indomethacin disrupts autophagic flux by disturbing the normal functioning of lysosomes and, by doing so, increases the sensitivity of gastric cancer cells to cytotoxic agents, an effect that could be used to overcome cancer cell resistance to antineoplastic regimes[4]. Concomitant administration of indomethacin (30 mg/kg) and curcumin resulted in a significantly reduced gastric damage compared to indomethacin alone[5]. Indomethacin treatment (i.p.) modulates microglia activation, contributing to increased neuroblast proliferation in the SVZ (subventricular zone) and migration to the ischaemic striatum following stroke[6].
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 数据源
143982 cells Function assay In vitro inhibitory activity against human Prostaglandin G/H synthase 2 (COX-2) in 143982 cells, IC50=9 nM 12877584
A549 cells 10 μM Function assay Inhibition of mPGES1 in human A549 cells assessed as inhibition of IL-1-beta-induced PGE2 formation at 10 uM by cell-intact assay 19053751
CHO cells Function assay In vitro inhibitory potency against human COX-1 in stably transfected chinese hamster ovary (CHO) cells, IC50=18 nM 10576684
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00811057 Preterm Labor Not Applicable Completed - United States, Mississippi ... 展开 >> The Winfred L. Wiser Hospital for Women and Infants at the University of Mississippi Medical Center Jackson, Mississippi, United States, 39216 收起 <<
NCT00811057 - Completed - -
NCT02609386 Squamous Cell Carcinoma of the... 展开 >> Oral Cavity 收起 << Phase 2 Active, not recruiting December 2019 United States, Arizona ... 展开 >> Banner University Medical Center Tucson, Arizona, United States, 85742 United States, Arkansas University of Arkansas For Medical Sciences Little Rock, Arkansas, United States, 72205 United States, California USC Norris Comprehensive Cancer Center Los Angeles, California, United States, 90033 Stanford University Medical Center Stanford, California, United States, 94305 United States, Georgia Emory University - Winship Cancer Center Atlanta, Georgia, United States, 30322 United States, Kentucky University of Kentucky Lexington, Kentucky, United States, 40506 United States, Michigan University of Michigan Ann Arbor, Michigan, United States, 48109 United States, Nebraska Nebraska Methodist Hospital Omaha, Nebraska, United States, 68114 United States, New York Monter Cancer Center - North Shore LIJ New Hyde Park, New York, United States, 11040 Lenox Hill Hospital New York, New York, United States, 10075 United States, Oklahoma University of Oklahoma Oklahoma City, Oklahoma, United States, 73104 United States, Oregon Providence Cancer Center Portland, Oregon, United States, 97209 United States, Pennsylvania Hospital of The University of Pennsylvania Philadelphia, Pennsylvania, United States, 19106 Brazil Hospital Erasto Gaertner Curitiba, Brazil Instituto Goiano de Oncologia e Hematologia (INGOH) Goiânia, Brazil Instituto do Câncer de Londrina Londrina, Brazil Instituto Nacional do Cancer (INCA) Rio de Janeiro, Brazil Hospital de Base de São José do Rio Preto São José do Rio Prêto, Brazil Instituto Brasileiro de Controle do Câncer São Paulo, Brazil Instituto do Cancer do Estado de São Paulo - ICESP São Paulo, Brazil Canada Sunnybrook Research Institute Toronto, Canada United Kingdom Queen Elizabeth University Hospital Glasgow Glasgow, United Kingdom 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.79mL

0.56mL

0.28mL

13.97mL

2.79mL

1.40mL

27.95mL

5.59mL

2.79mL
参考文献

[1]Hoehn BD, Palmer TD, et al. Neurogenesis in rats after focal cerebral ischemia is enhanced by indomethacin. Stroke. 2005 Dec;36(12):2718-24.

[2]Dihlmann S, Siermann A, et al. The nonsteroidal anti-inflammatory drugs aspirin and indomethacin attenuate beta-catenin/TCF-4 signaling. Oncogene. 2001 Feb 1;20(5):645-53.

[3]Riendeau D, Percival MD, Boyce S, Brideau C, Charleson S, Cromlish W, Ethier D, Evans J, Falgueyret JP, Ford-Hutchinson AW, Gordon R, Greig G, Gresser M, Guay J, Kargman S, Léger S, Mancini JA, O'Neill G, Ouellet M, Rodger IW, Thérien M, Wang Z, Webb JK, Wong E, Chan CC, et al. Biochemical and pharmacological profile of a tetrasubstituted furanone as a highly selective COX-2 inhibitor. Br J Pharmacol. 1997 May;121(1):105-17

[4]Vallecillo-Hernández J, Barrachina MD, Ortiz-Masiá D, Coll S, Esplugues JV, Calatayud S, Hernández C. Indomethacin Disrupts Autophagic Flux by Inducing Lysosomal Dysfunction in Gastric Cancer Cells and Increases Their Sensitivity to Cytotoxic Drugs. Sci Rep. 2018 Feb 26;8(1):3593

[5]Zazueta-Beltrán L, Medina-Aymerich L, Estela Díaz-Triste N, Chávez-Piña AE, Castañeda-Hernández G, Cruz-Antonio L. Evidence against the participation of a pharmacokinetic interaction in the protective effect of single-dose curcumin against gastrointestinal damage induced by indomethacin in rats. J Integr Med. 2017 Mar;15(2):151-157

[6]Lopes RS, Cardoso MM, Sampaio AO, Barbosa MS Jr, Souza CC, DA Silva MC, Ferreira EM, Freire MA, Lima RR, Gomes-Leal W. Indomethacin treatment reduces microglia activation and increases numbers of neuroblasts in the subventricular zone and ischaemic striatum after focal ischaemia. J Biosci. 2016 Sep;41(3):381-94