CP 80,633

Phosphodiesterases (PDE) enzymatically convert the cyclic nucleotide second messengers cAMP and cGMP to 5'-AMP and 5'-GMP, respectively, thus terminating signal transduction. The cAMP-specific PDE4 isoforms may be particularly important in certain respiratory and neurological diseases. CP 80,633 is a selective inhibitor of PDE4 (IC50 = 1.27 µM for PDE4 versus. >100 µM for PDE1, PDE2, PDE3, and PDE5). It potentiates PGE1-dependent increases in cAMP levels in eosinophils, monocytes, and T-cells, inhibits eosinophil superoxide production (IC50 induced TNF-alpha release from monocytes (IC50 = 0.22 µM). CP 80,633 (1 mg/kg) significantly reduces antigen-induced airway inflammation in atopic guinea pigs, monkeys, and mice.Formal Name: 5-[3-[(1S,2S,4R)-bicyclo[2.2.1]hept-2-yloxy]-methoxyphenyl]tetrahydro-2-(1H)-pyrimidinone. CAS Number: 135637-46-6. Molecular Formula: C18H24N2O3. Formula Weight: 316.4. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 3 mg/ml, DMF:PBS (pH 7) (1:10): 0.1 mg/ml, DMSO: 2 mg/ml. lambdamax: 230, 281 nm. SMILES: O=C(NC1)NCC1C2=CC(O[C@@H]3[C@H](C4)CC[C@H]4C3)=C(OC)C=C2. InChi Code: InChI=1S/C18H24N2O3/c1-22-15-5-4-12(14-9-19-18(21)20-10-14)8-17(15)23-16-7-11-2-3-13(16)6-11/h4-5,8,11,13-14,16H,2-3,6-7,9-10H2,1H3,(H2,19,20,21)/t11-,13+,16+/m1/s1. InChi Key: LITNEAPWQHVPOK-FFSVYQOJSA-N.