CAS:202409-33-4Etoricoxib

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Synonyms: MK-663;MK 0663

Etoricoxib is a selective COX2 inhibitor with IC50 of 1.1 ± 0.1 μM and 116 ± 8 μM for COX1.

规格	价格	促销价格	库存

18817579266

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18817579266

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实验数据

技术信息

CAS号

202409-33-4

储存条件

分子式

C18H15ClN2O2S

运输

蓝冰

分子量

358.84

别名

MK-663;MK 0663

溶解度

DMSO	500.0 mg/mL (1393.4 mM) warming
Water	insoluble

动物实验配方

IP	2% DMSO+2% Tween80+40% PEG300+water	10 mg/mL	clear
PO	0.5% CMC-Na	65 mg/mL	suspension

生物活性

靶点 COX2

IC50:1.1±0.1μM COX1

IC50:116±8μM
描述Etoricoxib is a novel orally active agent that selectively inhibits cyclooxygenase-2 (COX-2). Etoricoxib 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^[3]. Etoricoxib in 50 and 100 mg/kg doses changed the levels of oxidant/antioxidant parameters such as MDA, MPO, tGSH, GSHRd, GST, SOD, NO, and 8-OH/Gua in favour of antioxidants. Furthermore, etoricoxib prevented increase of COX-2 gene expression and ALT and AST levels^[4]. Etoricoxib 120 mg administered orally once daily has the same efficacy on acute gout as indometacin and diclofenac. Etoricoxib is tolerated better by patients than NSAIDs such as indometacin and diclofenac^[5].

靶点	Description	IC50
COX2		IC50:1.1±0.1μM
COX1		IC50:116±8μM