Indomethacin-Indometacin-DataSheet-生命科學(xué)試劑-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEIndomethacinCat. No.: HY-14397CAS No.: 53-86-1Synonyms: Indometacin分式: CHClNO分量: 357.79作靶點(diǎn): COX; Autophagy作通路: Immunology/Inflammation; Autophagy儲(chǔ)存式: 4C, protect from light* In solvent : -80C, 6 months; -20C, 1 month (protect fr

2、omlight)溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 100 mg/mL (279.49 mM; Need ultrasonic)H2O : 40% PEG300 5% Tween-80 45% salineSolubility: 7.5 mg/mL (20.96 mM); Clear solution2. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (6.99 mM); Clear solution3. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% corn oil1/3 Master of Small

3、 Molecules 您邊的抑制劑師www.MedChemESolubility: 7.5 mg/mL (20.96 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Indomethacin種有效的、選擇性的 COX1 和 COX2 抑制劑，在 CHO 細(xì)胞中，對(duì) COX-1 和 COX-2 的IC50 值分別為 18 nM 和 26 nM。IC50 & Target Human COX-1 Human COX-218 nM (IC50, in CHO cells) 26 nM (IC50, in CHO cells)體外研究 Indomethacin is

4、 a potent and nonselective inhibitor of COX1 and COX2, with IC50s of 18 nM and 26 nM forhuman COX-1 and COX-2, respectively, in CHO cells. Indomethacin inhibits lipopolysaccharide (LPS)-induced PGE2 production (COX-2) in a human whole blood assay with a potency (IC50=0.680.17M), andsuppresses coagul

5、ation-induced TXB2 production (COX-1) (IC50=0.190.02M). Indomethacin blocks COX-1 with an IC50 of 201nM in U937 cell microsomes at a low arachidonic acid concentration (0.1M) 1.體內(nèi)研究 Indomethacin dose-dependently inhibits both the carrageenan-induced rat paw oedema (ED50, 2.0mg/kg),hyperalgesia (ED50

6、, 1.5mg/kg), and is also effective at reversing LPS-induced pyrexia in rats (ED50, 1.1mg/kg) 1. Indomethacin (2.5 mg/kg, i.p) decreases the number of NeuN+ cells in the animals at 8 days afterET-1 injection. Indomethacin also reduces microglia/macrophage activation at 14 days. Indomethacinsignifican

7、tly increases the number of SVZ DCX+ cells/field at 14 days post stroke 2. Indomethacin (22.9mg/kg, p.o.) produces 8 to 10 linear mucosal lesions extended from the fundic to pyloric area of stomach wall3.PROTOCOLAnimal Rats 2Administration 2 To investigate the effects of Indomethacin treatment on bo

8、th microglia activation, neuroprotection and adultneurogenesis, rats are divided in four experimental groups: animals injected with ET-1, treated with sterilesaline (i.p.) for 7 days and perfused at 8 days following ET-1 injection (group 1, n=4); animals injected withET-1, treated with Indomethacin

9、(2.5 mg/kg, i.p) for 7 days and perfused at 8 days following ET-1 injection(group 2, n=4); animals injected with ET-1, treated with sterile saline (i.p.) for 7 days and perfused at 14 daysfollowing ET-1 injection (group 3, n=4); animals injected with ET-1, treated with Indomethacin (2.5 mg/kg, i.p)f

10、or 7 days and perfused at 14 days following ET-1 injection (group 4, n=4). After survival times of 7 or 14days, animals are deeply anesthetized with a mixture of ketamine hydrochloride (72 mg/kg, i.p.) and xylazinehydrochloride (9 mg/kg, i.p.). After the verification of complete absence of both the

11、corneal and the pawwithdraw reflexes, the animals are transcardially perfused with heparinized 0.9% warm phosphate-bufferedsaline (PBS) followed by 4% cold paraformaldehyde in 0.1 M phosphate buffer (PB), pH 7.4. Brains are post-fixed for 24 h in the same fixative and cryoprotected in different grad

12、ients of sucrose-glycerol solutions over 7days. The tissue is then frozen in an embedding medium, and cut at 30 M in the coronal plane using acryostat. Sections are then mounted onto gelatinized slides and stored in a freezer at 20C 2.MCE has not independently confirmed the accuracy of these methods

13、. They are for reference only.2/3 Master of Small Molecules 您邊的抑制劑師www.MedChemE戶使本產(chǎn)品發(fā)表的科研獻(xiàn) Chem Mater. 2017, 29(19):8221-8238. Int J Pharm. 2017 Jan 30;517(1-2):19-24. Toxicol Appl Pharmacol. 2017 Mar 22;323:44-52. Patent. US20180263995A1.See more customer validations on HYPERLINK / www.MedChemEREFE

14、RENCES1. Riendeau D, et al. Biochemical and pharmacological profile of a tetrasubstituted furanone as a highly selective COX-2 inhibitor. Br JPharmacol. 1997 May;121(1):105-17.2. Lopes RS, et al. Indomethacin treatment reduces microglia activation and increases numbers of neuroblasts in the subventr

15、icular zoneand ischaemic striatum after focal ischaemia. J Biosci. 2016 Sep;41(3):381-94.3. Afroz S, et al. Concentrated phosphatidic acid in cereal brans as potential protective agents against indomethacin-induced stomachulcer. J Agric Food Chem. 2016 Aug 26.4. Qixiong Zhang, et al. Structure-Property Correlations of Reactive Oxygen Species-Responsive and Hydrogen Peroxide-EliminatingMaterials with Anti-Oxidant and Anti-Inflammatory Activities. Che