吲哚美辛作用机制 - Medchemexpress - MCE中国

1、Product Data SheetIndomethacinCat. No.: HY-14397CAS No.: 53-86-1分式: CHClNO分量: 357.79作靶点: COX; Bacterial; Autophagy作通路: Immunology/Inflammation; Anti-infection; Autophagy储存式: 4C, protect from light* In solvent : -80C, 6 months; -20C, 1 month (protect from light)溶解性数据体外实验 DMSO : 100 mg/mL (279.49 mM;

2、Need ultrasonic)Ethanol : 12.5 mg/mL (34.94 mM; Need ultrasonic)H2O : 0.1 mg/mL (insoluble)SolventMass1 mg 5 mg 10 mgConcentration制备储备液1 mM 2.7949 mL 13.9747 mL 27.9494 mL5 mM 0.5590 mL 2.7949 mL 5.5899 mL10 mM 0.2795 mL 1.3975 mL 2.7949 mL请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存

3、式和期限：-80C, 6 months; -20C, 1 month (protect from light)。-80C 储存时，请在 6 个内使，-20C 储存时，请在 1 个内使。体内实验请根据您的实验动物和给药式选择适当的溶解案。以下溶解案都请先按照 In Vitro 式配制澄清的储备液，再依次添加助溶剂：为保证实验结果的可靠性，澄 的储备液可以根据储存条件，适当保存；体内实验的作液，建议您现现配，当天使； 以下溶剂前显的百分 指该溶剂在您配制终溶液中的体积占；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的式助溶1. 请依序添加每种溶剂： 10% DMSO 40% PEG30

4、0 5% Tween-80 45% salineSolubility: 7.5 mg/mL (20.96 mM); Clear solution此案可获得 7.5 mg/mL (20.96 mM，饱和度未知) 的澄清溶液。以 1 mL 作液为例，取 100 L 75.0 mg/mL 的澄 DMSO 储备液加到 400 L PEG300 中，混合均匀；向上述体系中加50 L Tween-80，混合均匀；然后继续加 450 L 理盐定容 1 mL。2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (6.99

5、 mM); Clear solution此案可获得 2.5 mg/mL (6.99 mM，饱和度未知) 的澄清溶液。Page 1 of 2 www.MedChemE以 1 mL 作液为例，取 100 L 25.0 mg/mL 的澄均匀。DMSO 储备液加到 900 L 20% 的 SBE-CD 理盐溶液中，混合3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 7.5 mg/mL (20.96 mM); Clear solution此案可获得 7.5 mg/mL (20.96 mM，饱和度未知) 的澄 溶液，此案不适于实验周 期在半个以上的实验。以 1

6、 mL 作液为例，取 100 L 75.0 mg/mL 的澄 DMSO 储备液加到 900 L 油中，混合均匀。4. 请依序添加每种溶剂： 10% EtOH 40% PEG300 5% Tween-80 45% salineSolubility: 1.25 mg/mL (3.49 mM); Clear solution此案可获得 1.25 mg/mL (3.49 mM，饱和度未知) 的澄清溶液。以 1 mL 作液为例，取 100 L 12.5 mg/mL 的澄 EtOH 储备液加到 400 L PEG300 中，混合均匀；向上述体系中加50 L Tween-80，混合均匀；然后继续加 450

7、L 理盐定容 1 mL。5. 请依序添加每种溶剂： 10% EtOH 90% (20% SBE-CD in saline)Solubility: 1.25 mg/mL (3.49 mM); Clear solution此案可获得 1.25 mg/mL (3.49 mM，饱和度未知) 的澄清溶液。以 1 mL 作液为例，取 100 L 12.5 mg/mL 的澄均匀。EtOH 储备液加到 900 L 20% 的 SBE-CD 理盐溶液中，混合6. 请依序添加每种溶剂： 10% EtOH 90% corn oilSolubility: 1.25 mg/mL (3.49 mM); Clear sol

8、ution此案可获得 1.25 mg/mL (3.49 mM，饱和度未知) 的澄 溶液，此案不适于实验周 期在半个以上的实验。以 1 mL 作液为例，取 100 L 12.5 mg/mL 的澄 EtOH 储备液加到 900 L 油中，混合均匀。BIOLOGICAL ACTIVITY物活性 Indomethacin (Indometacin) 种有效的、选择性的 COX1 和 COX2 抑制剂，在 CHO 细胞中，对 COX-1 和 COX-2 的 IC50 值分别为 18 nM 和 26 nM1。IC & Target Human COX-1 Human COX-218 nM (IC50, i

9、n CHO cells) 26 nM (IC50, in CHO cells)体外研究 Indomethacin is a potent and nonselective inhibitor of COX1 and COX2, with IC50s of 18 nM and 26 nM for humanCOX-1 and COX-2, respectively, in CHO cells. Indomethacin inhibits lipopolysaccharide (LPS)-induced PGE2production (COX-2) in a human whole blood a

10、ssay with a potency (IC50=0.680.17 M), and suppresses coagulation-induced TXB2 production (COX-1) (IC50=0.190.02 M). Indomethacin blocks COX-1 with an IC50 of 201 nM in U937cell microsomes at a low arachidonic acid concentration (0.1 M)1.体内研究 Indomethacin dose-dependently inhibits both the carrageen

11、an-induced rat paw oedema (ED50, 2.0 mg/kg),hyperalgesia (ED50, 1.5 mg/kg), and is also effective at reversing LPS-induced pyrexia in rats (ED50, 1.1 mg/kg)1.Indomethacin (2.5 mg/kg, i.p) decreases the number of NeuN+ cells in the animals at 8 days after ET-1 injection.Indomethacin also reduces micr

12、oglia/macrophage activation at 14 days. Indomethacin significantly increases thenumber of SVZ DCX+ cells/field at 14 days post stroke2. Indomethacin (22.9 mg/kg, p.o.) produces 8 to 10 linearmucosal lesions extended from the fundic to pyloric area of stomach wall3.PROTOCOLAnimal Rats2Page 2 of 3 www

13、.MedChemEAdministration 2 To investigate the effects of Indomethacin treatment on both microglia activation, neuroprotection and adultneurogenesis, rats are divided in four experimental groups: animals injected with ET-1, treated with sterile saline (i.p.)for 7 days and perfused at 8 days following

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

15、roup3, n=4); animals injected with ET-1, treated with Indomethacin (2.5 mg/kg, i.p) for 7 days and perfused at 14 daysfollowing ET-1 injection (group 4, n=4). After survival times of 7 or 14 days, animals are deeply anesthetized with amixture of ketamine hydrochloride (72 mg/kg, i.p.) and xylazine h

16、ydrochloride (9 mg/kg, i.p.). After the verification ofcomplete absence of both the corneal and the paw withdraw reflexes, the animals are transcardially perfused withheparinized 0.9% warm phosphate-buffered saline (PBS) followed by 4% cold paraformaldehyde in 0.1 M phosphatebuffer (PB), pH 7.4. Bra

17、ins are post-fixed for 24 h in the same fixative and cryoprotected in different gradients ofsucrose-glycerol solutions over 7 days. The tissue is then frozen in an embedding medium, and cut at 30 M in thecoronal plane using a cryostat. Sections are then mounted onto gelatinized slides and stored in

18、a freezer at 20C2.MCE has not independently confirmed the accuracy of these methods. They are for reference only.户使本产品发表的科研献 Chem Mater. 2017, 29(19):8221-8238. Int J Nanomedicine. 2020 May 1;15:3087-3098. Int J Pharm. 2017 Jan 30;517(1-2):19-24. Toxicol Appl Pharmacol. 2017 Mar 22;323:44-52. BMC Ca

19、ncer. 2019 Dec.See more customer validations on HYPERLINK www.MedChemE www.MedChemEREFERENCES1. Riendeau D, et al. Biochemical and pharmacological profile of a tetrasubstituted furanone as a highly selective COX-2 inhibitor. Br J Pharmacol. 1997May;121(1):105-17.2. Lopes RS, et al. Indomethacin treatment reduces microglia activation and increases numbers of neuroblasts in the subventricular zone and ischaemicstriatum after focal ischaemia. J Biosci. 20