A COX-1 inhibitor
Mofezolac is an inhibitor of COX-1 (IC50 = 14 nM).1 It is selective for COX-1 over COX-2 (IC50 = 440 nM). Mofezolac (1 ?g/ml) protects against LPS-induced cell death in BV-2 microglia. In vivo, mofezolac (6 mg/kg, i.p.) reduces hippocampal microglial activation and prostaglandin E2 production in a mouse model of LPS-induced neuroinflammation. It reduces phenylquinone-induced writhing in a mouse model of acute pain.2 Dietary administration of mofezolac (1,200 ppm) reduces the number of aberrant crypt foci and tumors in a rat model of beef tallow diet-induced colon carcinogenesis.3
1.Calvello, R., Lofrumento, D.D., Perrone, M.G., et al.Highly selective cyclooxygenase-1 inhibitors P6 and mofezolac counteract inflammatory state both in vitro and in vivo models of neuroinflammationFront. Neurol.8251(2017) 2.Goto, K., Ochi, H., Yasunaga, Y., et al.Analgesic effect of mofezolac, a non-steroidal anti-inflammatory drug, against phenylquinone-induced acute pain in miceProstaglandins Other Lipid Mediat.56(4)245-254(1998) 3.Miao, L., Shiraishi, R., Fujise, T., et al.Chemopreventive effect of mofezolac on beef tallow diet/azoxymethane-induced colon carcinogenesis in ratsHepatogastroenterology58(105)81-88(2011)
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