Tepoxalin

Tepoxalin is a dual inhibitor of COX and 5-lipoxygenase (5-LO, IC50s = 2.84 and 0.15 µM, respectively, in RBL-1 cell lysates). It also inhibits the activity of 12-, but not 15-, LO (IC50s = 4.45 and 146.6 µM for the human platelet and rabbit reticulocyte enzymes, respectively). Tepoxalin reduces the production of thromboxane B2 (TXB2, Cay-19030) and leukotriene B4 (LTB4, Cay-20110) induced by the calcium ionophore A23187 (Cay-11016, Cay-22030) in human peripheral blood mononuclear cells (PBMCs, IC50s = 0.01 and 0.07 µM, respectively) and decreases epinephrine-induced platelet aggregation in human platelet-rich plasma (PRP, IC50 = 0.045 µM). It inhibits paw swelling in a rat model of adjuvant-induced arthritis with an ED50 value of 3.5 mg/kg.Formal Name: 5-(4-chlorophenyl)-N-hydroxy-1-(4-methoxyphenyl)-N-methyl-1H-pyrazole-3-propanamide. CAS Number: 103475-41-8. Synonyms: ORF 20485, RWJ 20485. Molecular Formula: C20H20ClN3O3. Formula Weight: 385.8. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMF: 30 mg/ml, DMSO: 30 mg/ml, Ethanol: 15 mg/ml, PBS (pH 7.2): insolu. lambdamax: 237, 256 nm. SMILES: ClC(C=C1)=CC=C1C2=CC(CCC(N(O)C)=O)=NN2C3=CC=C(OC)C=C3. InChi Code: InChI=1S/C20H20ClN3O3/c1-23(26)20(25)12-7-16-13-19(14-3-5-15(21)6-4-14)24(22-16)17-8-10-18(27-2)11-9-17/h3-6,8-11,13,26H,7,12H2,1-2H3. InChi Key: XYKWNRUXCOIMFZ-UHFFFAOYSA-N.