SC57666是选择性的COX2抑制剂，IC50值为26nM。
SC57666 is a selective COX2 inhibitor with an IC50 of 26 nM.
SC57666 inhibits COX2 with an IC50 of 3.2±0.8 nM in CHO cells stably transfected with human COX isozymes, with 1000 fold or more selectivity over COX1 (IC50=6000±1900 nM)[2].
SC57666 has been shown to be orally active (ED50=1.7 mpk) in the adjuvant-induced arthritis model. No gastric lesions are observed in mice after 5 h when SC57666 is administered intragastrically at 600 mpk. No intestinal damage is observed in rats after 72 h when SC57666 is administered intragastrically at 200 mpk[1].
[1]. Reitz DB, et al. Selective cyclooxygenase inhibitors: novel 1,2-diarylcyclopentenes are potent and orally activeCOX2 inhibitors. J Med Chem. 1994 Nov 11;37(23):3878-81. [2]. Riendeau D, et al. Biochemical and pharmacological profile of a tetrasubstituted furanone as a highly selective COX2 inhibitor. Br J Pharmacol. 1997 May;121(1):105-17.
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