COX-2:1.1 μM (IC50, in human whole blood)
COX-1:116 μM (IC50, in human whole blood)
In Vivo
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 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 has little activity against COX-1 with a Ki of 167 μM[1].
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 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 has little activity against COX-1 with a Ki of 167 μM[1].
Kinase Assay
Cell Assay
Animal Administration
Rats[3] Animals are assorted into the following groups with four to six animals in each group: Control Group, Animals are 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 are administrated with DMH weekly at a dose of 30 mg/kg body weight subcutaneously, DMH is freshly prepared in 1mM EDTA-saline, pH adjusted to 7.0 using dilute NaOH solution; DMH + Etoricoxib Group, Etoricoxib is given daily per oral at its therapeutic anti-inflammatory dose (ED50 for rats, 0.64 mg/kg body weight) to the animals along with the weekly administration of DMH; and Etoricoxib Group: Etoricoxib alone is administered orally daily (0.64 mg/kg body weight). After six weeks, animals are kept on overnight fasting with drinking water ad libitum and sacrificed the next day. The animal body weights in all the groups are recorded once in a week till the termination.[3].
References
Rats[3] Animals are assorted into the following groups with four to six animals in each group: Control Group, Animals are 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 are administrated with DMH weekly at a dose of 30 mg/kg body weight subcutaneously, DMH is freshly prepared in 1mM EDTA-saline, pH adjusted to 7.0 using dilute NaOH solution; DMH + Etoricoxib Group, Etoricoxib is given daily per oral at its therapeutic anti-inflammatory dose (ED50 for rats, 0.64 mg/kg body weight) to the animals along with the weekly administration of DMH; and Etoricoxib Group: Etoricoxib alone is administered orally daily (0.64 mg/kg body weight). After six weeks, animals are kept on overnight fasting with drinking water ad libitum and sacrificed the next day. The animal body weights in all the groups are recorded once in a week till the termination.[3].
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