Cilomilast

Cilomilast is a second generation inhibitor of phosphodiesterase 4 (PDE4, IC50 = 0.12 µM for the human enzyme). It is selective for human PDE4 over bovine PDE1, rat PDE2, and human PDE3 and -5 (IC50s = 74, 65, >100, and 83 µM, respectively). Cilomilast inhibits LPS-induced production of TNF-alpha in isolated human monocytes, as well as decreases production of leukotriene B4 (LTB4, Cay-20110) induced by fMLP (Cay-21495) in isolated human neutrophils (IC50s = 110 and 40 nM, respectively). It reduces ovalbumin-induced bronchoconstriction and pulmonary eosinophil infiltration in an ovalbumin-sensitized guinea pig model of asthma when administered at doses of 10 and 30 mg/kg.Formal Name: cis-4-cyano-4-[3-(cyclopentyloxy)-4-methoxyphenyl]-cyclohexanecarboxylic acid. CAS Number: 153259-65-5. Synonyms: SB 207499. Molecular Formula: C20H25NO4. Formula Weight: 343.4. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMSO: 15mg/ml. lambdamax: 232 nm. SMILES: COC1=C(OC2CCCC2)C=C([C@@]3(C#N)CC[C@H](C(O)=O)CC3)C=C1. InChi Code: InChI=1S/C20H25NO4/c1-24-17-7-6-15(12-18(17)25-16-4-2-3-5-16)20(13-21)10-8-14(9-11-20)19(22)23/h6-7,12,14,16H,2-5,8-11H2,1H3,(H,22,23)/t14-,20?. InChi Key: CFBUZOUXXHZCFB-FZOZEDLRSA-N.