435801
Licofelone, Potassium Salt, Monohydrate
別名:
2,2-Dimethyl-6-(4-chlorophenyl)-7-phenyl, 2,3-dihydro-1H-pyrrolizine-5-yl)-acetic acid, ML3000, ML-3000, COX-1 Inhibitor V, FLAP Inhibitor II, mPGES-1 Inhibitor II
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この商品について
Form:
white powder
Solubility:
soluble (DMSO (100 mg/ml))
form
white powder
Quality Segment
storage condition
OK to freeze
solubility
soluble (DMSO (100 mg/ml))
storage temp.
−20°C
General description
A cell-permeable, orally active arylpyrrolizine carboxylate that is both structurally and pharmacologically similar to, but less potent than, MK-886 (Cat. No. 475889). Both MK-886 and Licofelone effectively suppress cellular Cox pathway PGE2 (prostaglandin E2) production by inhibiting COX-1 and mPGES-1 (microsomal PGE2 synthase-1), but not COX-2 (IC50 = 0.8, 6, and >30 µM, respectively, by Licofelone), and both compounds suppress cellular 5-LO (5-Lypoxygenase; Cat. No. 437996) pathway activation (IC50 = 0.18 to 3.6 µM against ionophore-stimulated bovine and human PMNL LB4 production by Licofelone) by inhibiting FLAP (5-LO-activating protein), rather than 5-LO, activity (No inhibition up to 10 µM Licofelone). Unlike NSAIDs (nonsteroidal antiinflammatory drugs) that target only COX pathway, Licofelone does not cause gastrointestinal damages when applied in vivo.