NS-398NS-398
MedChemExpress (MCE)
HY-13913
123653-11-2
99.72%
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Room temperature in continental US
may vary elsewhere.
NS-398 is a non-steroidal an-inflammatory agent with analgesic and antipyretic effects, and selectively inhibits prostaglandin G/H synthase 2/cyclooxygenase 2 (COX-2) activity, with an IC50 of 3.8 μM, and has no effect on COX-1 at 100 μM.
NS-398 is a non-steroidal an-inflammatory agent, selectively inhibits prostaglandin G/H synthase/cyclooxygenase (COX-2) activity, with an IC50 of 3.8 μM, and has no effect on COX-1 at 100 μM[1]. NS-398 weakly inhibits PG endoperoxide synthase activity from sheep seminal vesicle microsomes (IC50, 11 μM)[2].
NS-398 (0.5-10 mg/kg, p.o.) dose-dependently inhibits paw edema in rats, with an ED30 of 1.14 mg/kg, shows therapeutic 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, NS-398 suppresses writhing reactions induced by acetic acid with an ED50 of 8.2 mg/kg[2].
Mice[2] Briefly, male ddy mice weighing about 30 g are used. The writhing syndrome is induced by injecting 0.75% of acetic acid, intraperitoneally. Ten minutes later, the number of writhings 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[2] Briefly, male Lewis rats weighing about 160 g are used. Arthritis is induced by injecting 0.1 mL of 0.7% Mycobacterium tubercu-losis-liquid paraffin into the left hind paw. On day 15, the rats are grouped according to the degree of secondary lesions in the right hind paw. NS-398 is administered orally once daily from days 15 to 18. Foot volume is measured on day 19. Relative edema volume (REV) is calculated for each animal[2].
COX-2 3.8 μM (IC50)
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[1]. Futaki N, et al. NS-398, a new anti-inflammatory agent, selectively inhibits prostaglandin G/H synthase/cyclooxygenase (COX-2) activity in vitro. Prostaglandins. 1994 Jan
47(1):55-9. [Content Brief]
[2]. Futaki N, et al. NS-398, a novel non-steroidal anti-inflammatory drug with potent analgesic and antipyretic effects, which causes minimal stomach lesions. Gen Pharmacol. 1993 Jan
24(1):105-10. [Content Brief]