Diflapolin

Diflapolin is a dual inhibitor of 5-lipoxygenase-activating protein (FLAP) and soluble epoxide hydrolase (sEH). It inhibits formation of the 5-lipoxygenase (5-LO) products leukotriene B4 (LTB4, Cay-20110) and 5-HpETE (Cay-44230) in isolated human monocytes and neutrophils (IC50s = 30 and 170 nM, respectively) and inhibits the epoxide hydrolase activity of sEH with an IC50 value of 20 nM in a cell-free assay. It is selective for FLAP and sEH over other arachidonic acid metabolism enzymes, including 5-LO, LTC4 synthase, mPGES-1, COX-1, or COX-2 in cell-free assays, as well as 12- and 15-LO in neutrophils. Diflapolin (1, 3, and 10 mg/kg) decreases inflammation in a mouse model of peritonitis induced by zymosan, reducing the production of LTB4 and LTC4 and inhibiting leukocyte recruitment.Formal Name: N-[4-(2-benzothiazolylmethoxy)-2-methylphenyl]-N'-(3,4-dichlorophenyl)-urea. CAS Number: 724453-98-9. Molecular Formula: C22H17Cl2N3O2S. Formula Weight: 458.4. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 2.5mg/mL, DMSO: 1.6mg/mL. lambdamax: 259 nm. SMILES: CC1=C(NC(NC2=CC(Cl)=C(Cl)C=C2)=O)C=CC(OCC3=NC4=C(C=CC=C4)S3)=C1. InChi Code: InChI=1S/C22H17Cl2N3O2S/c1-13-10-15(29-12-21-26-19-4-2-3-5-20(19)30-21)7-9-18(13)27-22(28)25-14-6-8-16(23)17(24)11-14/h2-11H,12H2,1H3,(H2,25,27,28). InChi Key: FGXLEECGXSDIMM-UHFFFAOYSA-N.