Licofelone

Cross-talk between lipoxygenase (LO) and cyclooxygenase (COX) pathways has been observed in human osteoarthritic synovial explants which creates an arachidonic acid shunting phenomenon, stimulating interleukin-1beta (IL-1beta) synthesis. Licofelone is a dual inhibitor of cyclooxygenase (COX) and lipoxygenase (LO) pathways, that decreases levels of prostaglandin E2, leukotriene B4, and lipoxins and prevents lipopolysaccharide-stimulated IL-1beta expression. The IC50 values for inhibition of human thrombocyte COX and human 5-LO are 0.16 µM and 0.23 µM, respectively. Unlike other non-steroidal anti-inflammatory drugs, licofelone causes little or no damage to the gastric mucosa in rabbit parietal cells. This is presumably the result of licofelone's affects on acid-secretory mechanisms, mediated by the inhibition of 5-LO activity.Formal Name: 6-(4-chlorophenyl)-2,3-dihydro-2,2-dimethyl-7-phenyl-1H-pyrrolizine-5-acetic acid. CAS Number: 156897-06-2. Synonyms: ML 3000. Molecular Formula: C23H22ClNO2. Formula Weight: 379.9. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 20 mg/ml, DMSO: 20 mg/ml, DMSO:PBS (pH 7.2) (1:8): .5 mg/ml, Ethanol: 5 mg/ml. lambdamax: 248, 278 nm. SMILES: CC1(C)CC2=C(C3=CC=CC=C3)C(C4=CC=C(Cl)C=C4)=C(CC(O)=O)N2C1. InChi Code: InChI=1S/C23H22ClNO2/c1-23(2)13-19-22(15-6-4-3-5-7-15)21(16-8-10-17(24)11-9-16)18(12-20(26)27)25(19)14-23/h3-11H,12-14H2,1-2H3,(H,26,27). InChi Key: UAWXGRJVZSAUSZ-UHFFFAOYSA-N.