Roflumilast N-oxide

Roflumilast N-oxide is an inhibitor of phosphodiesterase 4 (PDE4, IC50 = 2 nM) and an active metabolite of the PDE4 inhibitor roflumilast (Cay-15141). It is selective for PDE4 over PDE1-3 and PDE5 (IC50s = >10,000 nM for all). It reduces TNF-alpha-induced ICAM-1 and eotaxin levels when used in combination with prostaglandin E2 (PGE2, Cay-14010) in GM06114 human fetal lung fibroblasts (IC50s = 0.9 and 0.5 nM, respectively). It also reduces bFGF-induced and IL-1beta augmented proliferation in the same cells. Roflumilast N-oxide (2 nM) reverses cigarette smoke extract-induced reductions in ciliary beat frequency in isolated human bronchial epithelial cells. Roflumilast N-oxide also increases plasma glucagon-like peptide 1 (GLP-1) levels in a glucose challenge in diabetic db/db mice when administered at a dose of 10 mg/kg, as well as prevents increases in blood glucose in db/db mice at 3 mg/kg per day.Formal Name: 3-(cyclopropylmethoxy)-N-(3,5-dichloro-1-oxido-4-pyridinyl)-4-(difluoromethoxy)-benzamide. CAS Number: 292135-78-5. Molecular Formula: C17H14Cl2F2N2O4. Formula Weight: 419.2. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMF: 30 mg/ml, DMSO: 30 mg/ml, Ethanol: 5 mg/ml. lambdamax: 214, 231, 288 nm. SMILES: FC(F)OC(C=C1)=C(C=C1C(NC(C(Cl)=C[N](=O)=C2)=C2Cl)=O)OCC3CC3. InChi Code: InChI=1S/C17H14Cl2F2N2O4/c18-11-6-23(25)7-12(19)15(11)22-16(24)10-3-4-13(27-17(20)21)14(5-10)26-8-9-1-2-9/h3-7,9,17H,1-2,8H2,(H,22,24). InChi Key: PCGSQNPMMSALEJ-UHFFFAOYSA-N.