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Etoricoxib

Chemical Structure : Etoricoxib

CAS No.: 202409-33-4

Etoricoxib (MK-0663, MK0663)

Catalog No.: PC-20873Not For Human Use, Lab Use Only.

Etoricoxib (MK-0663) is a potent, selective and orally active inhibitor of COX-2 with IC50 of 1.1 uM for COX-2 (LPS-induced prostaglandin E2 synthesis), shows no activity against COX-1.

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Biological Activity

Etoricoxib (MK-0663) is a potent, selective and orally active inhibitor of COX-2 with IC50 of 1.1 uM for COX-2 (LPS-induced prostaglandin E2 synthesis), shows no activity against COX-1.
Etoricoxib does not inhibit platelet or human recombinant COX-1 under most assay conditions (IC50>100 uM).
Etoricoxib is a potent inhibitor in models of carrageenan-induced paw edema (ID(50) 0.64 mg/kg), carrageenan-induced paw hyperalgesia (ID(50)=0.34 mg/kg), LPS-induced pyresis (ID(50) = 0.88 mg/kg), and adjuvant-induced arthritis (ID(50)=0.6 mg/kg/day) in rats.
Etoricoxib reversed LPS-induced pyresis by 81% within 2 h of administration at a dose of 3 mg/kg and showed no effect in a fecal 51Cr excretion model of gastropathy at 100 mg/kg/day for 5 days.

Physicochemical Properties

M.Wt 358.84
Formula C18H15ClN2O2S
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

5-chloro-2-(6-methylpyridin-3-yl)-3-(4-methylsulfonylphenyl) pyridine

References

1. Riendeau D, et al. J Pharmacol Exp Ther. 2001 Feb;296(2):558-66.

2. Chauret N, et al. Bioorg Med Chem Lett. 2001 Apr 23;11(8):1059-62.

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