Diclofenac-diethylamine _COX 抑制劑 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEDiclofenac diethylamineCat. No.: HY-15036ACAS No.: 78213-16-8分式: CHClNO分量: 369.29作靶點: COX作通路: Immunology/Inflammation儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實驗 DMSO : 150 mg/mL (406.18 mM; Ne

2、ed ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 2.7079 mL 13.5395 mL 27.0790 mL5 mM 0.5416 mL 2.7079 mL 5.4158 mL10 mM 0.2708 mL 1.3539 mL 2.7079 mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存式和期限。體內(nèi)實驗 請根據(jù)您的實驗動物和給藥式選擇適當(dāng)?shù)娜芙獍?，配制前請先配制澄清的儲備液，再依次添加助溶?為保證實驗結(jié)果的可靠性，體內(nèi)實驗的作液，建議您現(xiàn)現(xiàn)配，當(dāng)天使；澄清的儲備液可以根據(jù)

3、儲存條件，適當(dāng)保存；以下溶劑前的百分 指該溶劑在您配制終溶液中的體積占)：1. 請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (6.77 mM); Clear solution2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (6.77 mM); Clear solution3. 請依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (6.77 m

4、M); Clear solution1/3 Master of Small Molecules 您邊的抑制劑師www.MedChemEBIOLOGICAL ACTIVITY物活性 Diclofenac diethylamine種有效的，選擇性的抗炎劑，為 COX 的抑制劑，在 CHO 細胞中，對 COX-1和 COX-2 的 IC50 值分別為 4 nM，1.3 nM；Diclofenac diethylamine 同時對綿 COX-1 和 COX-2 的 IC50 值分別為 5.1 M，0.84 M。IC50 & Target Human COX-2 Human COX-1 Ovine CO

5、X-2 Ovine COX-11.3 nM (IC50, in CHO 4 nM (IC50, in CHO 0.84 M (IC50) 5.1 M (IC50)cells) cells)體外研究 Diclofenac diethylamine is a potent COX inhibitor, with IC50s of 4 nM and 1.3 nM for human COX-1 andCOX-2 in the CHO cells, respectively. Diclofenac effectively blocks COX-1 mediated prostanoid product

6、ionfrom U937 cell microsomes, with an IC50 of 7 3 nM 1. Diclofenac sodium exihibits inhibition on COX-1and COX-2 enzyme with IC50s of 5.1 and 0.84 M, respectively 2.體內(nèi)研究 Diclofenac (3 mg/kg, b.i.d., for 5 days) significantly increases faecal 51Cr excretion in rats, and such effect isalso observed in

7、 squirrel monkeys after administrated of 1 mg/kg twice daily for 4 days 1. Diclofenac (10mg/kg) shows anti-inflammatory activity in mice 2. Diclofenac (10 mg/kg) decreases oxidized low-densitylipoprotein (Ox-LDL), but shows no effects on the kinetics parameters of catalase and glutathioneperoxidase

8、via intramuscularly injection into rats 3.PROTOCOLAnimal Rats 1Administration 1 Male Sprague-Dawley rats (150 200 g) are dosed orally with Diclofenac either once (acute dosing) or twicedaily for 5 days (chronic dosing). A plasma sample is obtained 1 h after the morning dose on day 4 formeasurement o

9、f Diclofenac concentration. Immediately after the administration of the last dose on day 5, therats are injected via a tail vein with 0.5 mL of 51Cr-labelled red blood cells from a donor rat after incubationwith sodium 51chromate. The rats are placed individually in metabolism cages with food and wa

10、ter adlibitum. Faeces are collected for a 48 h period and 51Cr faecal excretion is calculated as a % of total injecteddose (20 mCi per animal) 1.Squirrel monkeys 1Squirrel monkeys (Saimiri sciureus; 0.8 1.4 kg) are dosed orally with Diclofenac twice daily for 1 5 days.One hour after administration o

11、f the last dose, 51CrCl3 in sterile saline (1 mL/kg, 4 5 mCi per animal) isinjected via a saphenous vein and plasma samples are obtained for measurement of Diclofenacconcentration. The monkeys are then housed individually in metabolism cages. Faeces are collected for a 24h period and 51Cr faecal exc

12、retion is calculated as a % of total injected dose 1.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 J Hazard Mater. 2015 May 30;289:18-27.2/3 Master of Small Molecules 您邊的抑制劑師www.MedChemE Chemosphere. 2019 Mar. Phys Chem Chem Phys. 2016 Jan

13、 21;18(3):1526-36. J Phys Chem Solids. 2017 October;109:117-123. Toxicol Mech Methods. 2019 Jul 25:1-24.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Riendeau D, et al. Biochemical and pharmacological profile of a tetrasubstituted furanone as a highly selective COX-2 inhibito

14、r. Br JPharmacol. 1997 May;121(1):105-17.2. Labib MB, et al. Design, synthesis of novel isoindoline hybrids as COX-2 inhibitors: Anti-inflammatory, analgesic activities and dockingstudy. Bioorg Chem. 2018 Oct;80:70-80.3. Curcelli EC, et al. Beneficial effects of diclofenac therapy on serum lipids, oxidized low-density lipoprotein and antioxidant defenses inrats. Life Sci. 2008 Apr 9;82(