1、Product Data SheetIndomethacinCat. No.: HY-14397CAS No.: 53-86-1分式: CHClNO分量: 357.79作靶點(diǎn): COX; Bacterial; Autophagy作通路: Immunology/Inflammation; Anti-infection; Autophagy儲(chǔ)存式: 4C, protect from light* In solvent : -80C, 6 months; -20C, 1 month (protect from light)溶解性數(shù)據(jù)體外實(shí)驗(yàn) 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制備儲(chǔ)備液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請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲(chǔ)備液的保存

3、式和期限：-80C, 6 months; -20C, 1 month (protect from light)。-80C 儲(chǔ)存時(shí)，請(qǐng)?jiān)?6 個(gè)內(nèi)使，-20C 儲(chǔ)存時(shí)，請(qǐng)?jiān)?1 個(gè)內(nèi)使。體內(nèi)實(shí)驗(yàn)請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥式選擇適當(dāng)?shù)娜芙獍浮Ｒ韵氯芙獍付颊?qǐng)先按照 In Vitro 式配制澄清的儲(chǔ)備液，再依次添加助溶劑：為保證實(shí)驗(yàn)結(jié)果的可靠性，澄 的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的作液，建議您現(xiàn)現(xiàn)配，當(dāng)天使； 以下溶劑前顯的百分 指該溶劑在您配制終溶液中的體積占；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的式助溶1. 請(qǐng)依序添加每種溶劑： 10% DMSO 40% PEG30

4、0 5% Tween-80 45% salineSolubility: 7.5 mg/mL (20.96 mM); Clear solution此案可獲得 7.5 mg/mL (20.96 mM，飽和度未知) 的澄清溶液。以 1 mL 作液為例，取 100 L 75.0 mg/mL 的澄 DMSO 儲(chǔ)備液加到 400 L PEG300 中，混合均勻；向上述體系中加50 L Tween-80，混合均勻；然后繼續(xù)加 450 L 理鹽定容 1 mL。2. 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

5、 mM); Clear solution此案可獲得 2.5 mg/mL (6.99 mM，飽和度未知) 的澄清溶液。Page 1 of 2 www.MedChemE以 1 mL 作液為例，取 100 L 25.0 mg/mL 的澄均勻。DMSO 儲(chǔ)備液加到 900 L 20% 的 SBE-CD 理鹽溶液中，混合3. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 7.5 mg/mL (20.96 mM); Clear solution此案可獲得 7.5 mg/mL (20.96 mM，飽和度未知) 的澄 溶液，此案不適于實(shí)驗(yàn)周 期在半個(gè)以上的實(shí)驗(yàn)。以 1

6、 mL 作液為例，取 100 L 75.0 mg/mL 的澄 DMSO 儲(chǔ)備液加到 900 L 油中，混合均勻。4. 請(qǐng)依序添加每種溶劑： 10% EtOH 40% PEG300 5% Tween-80 45% salineSolubility: 1.25 mg/mL (3.49 mM); Clear solution此案可獲得 1.25 mg/mL (3.49 mM，飽和度未知) 的澄清溶液。以 1 mL 作液為例，取 100 L 12.5 mg/mL 的澄 EtOH 儲(chǔ)備液加到 400 L PEG300 中，混合均勻；向上述體系中加50 L Tween-80，混合均勻；然后繼續(xù)加 450

7、L 理鹽定容 1 mL。5. 請(qǐng)依序添加每種溶劑： 10% EtOH 90% (20% SBE-CD in saline)Solubility: 1.25 mg/mL (3.49 mM); Clear solution此案可獲得 1.25 mg/mL (3.49 mM，飽和度未知) 的澄清溶液。以 1 mL 作液為例，取 100 L 12.5 mg/mL 的澄均勻。EtOH 儲(chǔ)備液加到 900 L 20% 的 SBE-CD 理鹽溶液中，混合6. 請(qǐng)依序添加每種溶劑： 10% EtOH 90% corn oilSolubility: 1.25 mg/mL (3.49 mM); Clear sol

8、ution此案可獲得 1.25 mg/mL (3.49 mM，飽和度未知) 的澄 溶液，此案不適于實(shí)驗(yàn)周 期在半個(gè)以上的實(shí)驗(yàn)。以 1 mL 作液為例，取 100 L 12.5 mg/mL 的澄 EtOH 儲(chǔ)備液加到 900 L 油中，混合均勻。BIOLOGICAL ACTIVITY物活性 Indomethacin (Indometacin) 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 nM1。IC & Target Human COX-1 Human COX-218 nM (IC50, i

9、n CHO cells) 26 nM (IC50, in CHO cells)體外研究 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.體內(nèi)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.戶使本產(chǎn)品發(fā)表的科研獻(xiàn) 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