Etoricoxib-MK-0663-DataSheet-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEEtoricoxibCat. No.: HY-15321CAS No.: 202409-33-4Synonyms: MK-0663; L-791456分式: CHClNOS分量: 358.84作靶點(diǎn): COX作通路: Immunology/Inflammation儲(chǔ)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(shí)驗(yàn) DMSO : 100 mg/mL

2、 (278.68 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液1 mM 2.7868 mL 13.9338 mL 27.8676 mL5 mM 0.5574 mL 2.7868 mL 5.5735 mL10 mM 0.2787 mL 1.3934 mL 2.7868 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，并請(qǐng)注意儲(chǔ)備液的保存式和期限。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)娜芙獍福渲魄罢?qǐng)先配制澄清的儲(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，體內(nèi)實(shí)驗(yàn)的作液，建議您現(xiàn)現(xiàn)配，

3、當(dāng)天使；澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)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(qǐng)依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (6.97 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 (6.97 mM); Clear solution3. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% corn oil1/3 Master of S

4、mall Molecules 您邊的抑制劑師www.MedChemESolubility: 2.5 mg/mL (6.97 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Etoricoxib (MK-0663)種甾體抗炎劑，為可服的、選擇性的 COX-2 抑制劑，對(duì)全 COX-2 和 COX-1 的 IC50 值分別為 1.1 M 和 116 M。IC50 & Target COX-2 COX-11.1 M (IC50, in human whole blood) 116 M (IC50, in human whole blood)體外研究 Etorico

5、xib (MK-0663) is a selective and orally active COX-2 inhibitor, with IC50s of 1.1 M, 116 M and 5 Mfor COX-2, COX-1 in human whole blood and purified human COX-2, respectively. Etoricoxib (MK-0663)shows inhibitory effect on PGE2 production by CHO (COX-2) cells (IC50, 79 nM), on purified human COX-2wi

6、th detergent (IC50, 4.1 M), and on purified PGE2 production by U937 microsomes (low substrate; IC50,12.1 M). However, Etoricoxib (MK-0663) has little activity against COX-1 with a Ki of 167 M 1.體內(nèi)研究 Etoricoxib (MK-0663) (0.1-30 mg/kg, p.o.) dose-dependently inhibits carrageenan-induced paw edema,car

7、rageenan-induced paw hyperalgesia, and endotoxin-induced pyresis in rats. Etoricoxib (10 mg/kg)completely reverses hyperalgesia response in the rat hyperalgesia model. Etoricoxib (MK-0663) (200mg/kg/day) has no effect on urinary 51Cr excretion in rats, and nor in monkeys at 100 mg/kg/day 1.Etoricoxi

8、b (MK-0663) (50 and 100mg/kg) potently increases the malondialdehyde (MDA) andmyeloperoxidase (MPO) levels, and decreases the total glutathione (tGSH) and glutathione reductase(GSHRd) levels in rats. Etoricoxib (MK-0663) (100mg/kg) significantly inhibits the decrease of NO in rats 2.Etoricoxib (MK-0

9、663) (0.64 mg/kg, p.o.) reduces the features such as multiple plaque lesions, hyperplasiaand dysplasia induced by 1,2-dimethylhydrazine dihydrochloride (DMH) in rats 3.PROTOCOLAnimal Rats 3Administration 3 Animals are assorted into the following groups with four to six animals in each group: Control

10、 Group, Animalsare administrated the vehicle (1mM EDTA-saline subcutaneously) in weekly injection and 0.5%carboxymethyl cellulose per oral daily; 1,2-dimethylhydrazine dihydrochloride (DMH) Group, animals areadministrated with DMH weekly at a dose of 30 mg/kg body weight subcutaneously, DMH is fresh

11、ly preparedin 1mM EDTA-saline, pH adjusted to 7.0 using dilute NaOH solution; DMH + Etoricoxib Group, Etoricoxib(MK-0663) is given daily per oral at its therapeutic anti-inflammatory dose (ED50 for rats, 0.64 mg/kg bodyweight) to the animals along with the weekly administration of DMH; and Etoricoxi

12、b Group: Etoricoxib (MK-0663) alone is administered orally daily (0.64 mg/kg body weight). After six weeks, animals are kept onovernight fasting with drinking water ad libitum and sacrificed the next day. The animal body weights in all thegroups are recorded once in a week till the termination. 3.MC

13、E has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES2/3 Master of Small Molecules 您邊的抑制劑師www.MedChemE1. Riendeau D, et al.Etoricoxib (MK-0663): preclinical profile and comparison with other agents that selectively inhibit cyclooxygenase-2. JPharmaco

14、l Exp Ther. 2001 Feb;296(2):558-66.2. Kunak CS, et al. The Effect of Etoricoxib on Hepatic Ischemia-Reperfusion Injury in Rats. Oxid Med Cell Longev. 2015;2015:598162.3. Tanwar L, et al. Anti-proliferative and apoptotic effects of etoricoxib, a selective COX-2 inhibitor, on 1,2-dimethylhydrazinedihydrochloride-induced colon carcinogenesis. Asian Pac J Cancer Prev. 2010;11