Roflumilast

Roflumilast is an inhibitor of phosphodiesterase 4 (PDE4, IC50 = 0.8 nM). It is selective for PDE4 over PDE1, -2, -3, and -5 (IC50s = >10, >10, >10, and 8 µM, respectively). Roflumilast inhibits the production of leukotriene B4 (LTB4, Cay-20110) induced by fMLP (Cay-21495) in isolated human neutrophils with an IC50 value of 2 nM. It reduces the proliferation of anti-CD3 and anti-CD28-stimulated isolated human CD4+ T cells (IC30 = 7 nM). Roflumilast (5 mg/kg) prevents pulmonary inflammatory cell infiltration and emphysema in mice exposed to cigarette smoke. Formulations containing roflumilast have been used in the treatment of chronic obstructive pulmonary disease (COPD).Formal Name: 3-(cyclopropylmethoxy)-N-(3,5-dichloro-4-pyridinyl)-4-(difluoromethoxy)-benzamide. CAS Number: 162401-32-3. Synonyms: B 9302-107, BY 217, BYK 20869. Molecular Formula: C17H14Cl2F2N2O3. Formula Weight: 403.2. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMF:PBS (pH 7.2) (1:3): 0.25 mg/ml, DMSO: 20 mg/ml, Ethanol: 10 mg/ml. lambdamax: 212, 250 nm. SMILES: FC(F)OC1=C(OCC2CC2)C=C(C(NC3=C(Cl)C=NC=C3Cl)=O)C=C1. InChi Code: InChI=1S/C17H14Cl2F2N2O3/c18-11-6-22-7-12(19)15(11)23-16(24)10-3-4-13(26-17(20)21)14(5-10)25-8-9-1-2-9/h3-7,9,17H,1-2,8H2,(H,22,23,24). InChi Key: MNDBXUUTURYVHR-UHFFFAOYSA-N.