Vioxx Inhibitor CAS No. 162011-90-7

Cat. No.	Name	Size	Price	Add Cart
KI0862	Vioxx	50 mg	$154

Chemical Characteristic

Product Name	Vioxx
Synonyms	rofecoxib,Ceoxx, Ceeoxx, MK-0966
CAS No.	162011-90-7
Molecular Weight	314.36
Formula	C₁₇H₁₄O₄S
Chemical Structure

Biological activities

Vioxx is a highly selective inhibitor of cyclooxygenase-2 (COX-2). The IC50 of vioxx is 0.196 µM against COX-2. In contrast, vioxx inhibits COX-1 with an IC50 of 159.7 µM.^[1] Vioxx inhibits the COX-2-dependent production of PGE2 in human osteosarcoma cells and Chinese hamster ovary cells expressing human COX-2 with IC50 of 26 and 18 nM, respectively. In an in vitro human whole blood assay, vioxx selectively inhibits lipopolysaccharide-induced, COX-2-derived PGE2 synthesis with an IC50 value of 0.53 µM compared with an IC50 value of 18.8 µM for the inhibition of COX-1-derived thromboxane B2 synthesis after blood coagulation.^[2] Vioxx moderately prevents phenacetin O-deethylation with an IC50 of 23.0 µM.^[3] Vioxx produces significant but small delay in the onset of locomotor impairment in mice at the dose of 10 mg/kg of weight.^[4]

Protocols

In vitro: Vioxx is dissolved in DMSO (1% v/v). ^[3]

References

[1] Habeeb AG, et al. Design and synthesis of celecoxib and rofecoxib analogues as selective cyclooxygenase-2 (COX-2) inhibitors: replacement of sulfonamide and methylsulfonyl pharmacophores by an azido bioisostere. J Med Chem. 2001, 44(18): 3039-3042. 閵嗏偓閵嗏偓 [2] Chan CC, et al. Rofecoxib [Vioxx, MK-0966; 4-(4'-methylsulfonylphenyl)-3-phenyl-2-(5H)-furanone]: a potent and orally active cyclooxygenase-2 inhibitor. Pharmacological and biochemical profiles. J Pharmacol Exp Ther. 1999, 290(2): 551-560. 閵嗏偓閵嗏偓 [3] Karjalainen MJ, et al. Rofecoxib is a potent, metabolism-dependent inhibitor of CYP1A2: implications for in vitro prediction of drug interactions. Drug Metab Dispos. 2006, 34(12): 2091-2096. 閵嗏偓閵嗏偓 [4] Azari MF, et al. Effects of intraperitoneal injection of Rofecoxib in a mouse model of ALS. Eur J Neurol. 2005, 12(5): 357-364. 閵嗏偓閵嗏偓

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