Etoricoxib

Etoricoxib (MK-0663) selectively inhibited COX-2 in human whole blood assays in vitro, with an IC50 value of 1.1 ± 0.1 μM for COX-2 (LPS-induced prostaglandin E2 synthesis), compared with an IC50 value of 116 ± 8 μM for COX-1 (serum thromboxane B2 generation after clotting of the blood) . (In Vitro) :Etoricoxib (MK-0663) is a selective and orally active COX-2 inhibitor, with IC50s of 1.1 μM, 116 μM and 5 μM for 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-2 with detergent (IC50, 4.1 μM), and on purified PGE2 production by U937 microsomes (low substrate; IC50, 12.1 μM) . However, Etoricoxib (MK-0663) has little activity against COX-1 with a Ki of 167 μM. (In Vivo) :Etoricoxib (MK-0663) (0.1-30 mg/kg, p.o.) dose-dependently inhibits carrageenan-induced paw edema, carrageenan-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) (200 mg/kg/day) has no effect on urinary 51Cr excretion in rats, and nor in monkeys at 100 mg/kg/day. Etoricoxib (MK-0663) (50 and 100 mg/kg) potently increases the malondialdehyde (MDA) and myeloperoxidase (MPO) levels, and decreases the total glutathione (tGSH) and glutathione reductase (GSHRd) levels in rats. Etoricoxib (MK-0663) (100 mg/kg) significantly inhibits the decrease of NO in rats. Etoricoxib (MK-0663) (0.64 mg/kg, p.o.) reduces the features such as multiple plaque lesions, hyperplasia and dysplasia induced by 1,2-dimethylhydrazine dihydrochloride (DMH) in rats.

202409-33-4

L-791,456 | MK-0663

Pharmacology & Drug Discovery

>98% (HPLC)

Soluble in DMSO

O=S (C1=CC=C (C2=CC (Cl) =CN=C2C3=CC=C (C) N=C3) C=C1) (C) =O

C18H15ClN2O2S

358.84

Storage temperature: -20°C. Stability: ≥ 2 years

For research use only.