Piclamilast

Piclamilast is a phosphodiesterase 4 (PDE4) inhibitor (IC50 = 0.31 nM). It is selective for PDE4 over PDE1, PDE2, PDE3, PDE5, and PDE7A in cell-free assays (IC50s = >100, 40, >100, 14, and >10 µM, respectively). Piclamilast inhibits superoxide production by guinea pig eosinophils and histamine-induced contraction in isolated guinea pig trachea (IC50s = 24 and 2 nM, respectively). It inhibits eosinophil, neutrophil, lymphocyte, and TNF-alpha accumulation in bronchoalveolar lavage fluid (BALF) from ovalbumin-sensitized rats (ED50s = 23.8, 14.1, 19.5, and 14.4 µmol/kg, respectively). Piclamilast also inhibits ovalbumin-induced bronchoconstriction in a guinea pig model of asthma (ED50 = 0.033 mg/kg).Formal Name: 3-(cyclopentyloxy)-N-(3,5-dichloro-4-pyridinyl)-4-methoxy-benzamide. CAS Number: 144035-83-6. Synonyms: RP 73401, RPR 73401. Molecular Formula: C18H18Cl2N2O3. Formula Weight: 381.3. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMSO: 100 mM, Ethanol: 20 mM. SMILES: ClC1=C(NC(C2=CC(OC3CCCC3)=C(OC)C=C2)=O)C(Cl)=CN=C1. InChi Code: InChI=1S/C18H18Cl2N2O3/c1-24-15-7-6-11(8-16(15)25-12-4-2-3-5-12)18(23)22-17-13(19)9-21-10-14(17)20/h6-10,12H,2-5H2,1H3,(H,21,22,23). InChi Key: RRRUXBQSQLKHEL-UHFFFAOYSA-N.