1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemENS-398Cat. No.: HY-13913CAS No.: 123653-11-2分式: CHNOS分量: 314.36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 : 9 mg/mL (28.63 mM; Need ultrasonic and war

2、ming)H2O : 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (7.95 mM); Suspended solution; Need ultrasonicBIOLOGICAL ACTIVITY1/3 Master of Small Molecules 您邊的抑制劑師www.MedChemE物活性 NS-398種甾體類抗炎劑，具有鎮(zhèn)痛解熱作；NS-398 能夠選擇性地抑制 COX-2 的活性，IC50 值為 3.8M，在 100 M 的濃度下，對(duì) COX-1 的活性沒有作。IC50 & Target COX-23.8 M (IC50)體外研

3、究 NS-398 is a non-steroidal an-inflammatory agent, selectively inhibits prostaglandin G/Hsynthase/cyclooxygenase (COX-2) activity, with an IC50 of 3.8 M, and has no effect on COX-1 at 100 M 1.NS-398 weakly inhibits PG endoperoxide synthase activity from sheep seminal vesicle microsomes (IC50, 11M) 2

4、.體內(nèi)研究 NS-398 (0.5-10 mg/kg, p.o.) dose-dependently inhibits paw edema in rats, with an ED30 of 1.14 mg/kg, showstherapeutic effects on adjuvant arthritis (ED30, 4.69 mg/kg), exhibits dose-dependent analgesic activity (ED50,1.65 mg/kg), and has antipyretic effect (ED50, 1.84 mg/kg) in rats. In mice,

5、NS-398 suppresses writhingreactions induced by acetic acid with an ED50 of 8.2 mg/kg 2.PROTOCOLAnimal Mice 2Administration 2 Briefly, male ddy mice weighing about 30 g are used. The writhing syndrome is induced by injecting 0.75% ofacetic acid, intraperitoneally. Ten minutes later, the number of wri

6、things are counted for the next 10 min. NS-398 is administered orally 30 min prior to the injection. The analgesic effect is expressed as % of inhibition,compared with the vehicle-treated control 2.Rats 2Briefly, male Lewis rats weighing about 160 g are used. Arthritis is induced by injecting 0.1 mL

7、 of 0.7%Mycobacterium tubercu-losis-liquid paraffin into the left hind paw. On day 15, the rats are grouped accordingto the degree of secondary lesions in the right hind paw. NS-398 is administered orally once daily from days15 to 18. Foot volume is measured on day 19. Relative edema volume (REV) is

8、 calculated for each animal2.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) EBioMedicine. 2019 Jul;45:341-350.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Futaki N, et al. NS-398, a new anti-inflammatory agent, sele

9、ctively inhibits prostaglandin G/H synthase/cyclooxygenase (COX-2) activityin vitro. Prostaglandins. 1994 Jan;47(1):55-9.2. Futaki N, et al. NS-398, a novel non-steroidal anti-inflammatory drug with potent analgesic and antipyretic effects, which causes minimalstomach lesions. Gen Pharmacol. 1993 Jan;24(1):105-10.2/3 Master of Small Molecules 您邊的抑制劑師www.MedChemEMcePdfHeightCaution: Product has not been fully validated for me