GSK356278

GSK356278 is a potent, selective, and orally bioavailable phosphodiesterase 4 (PDE4) inhibitor with anxiolytic and cognition-improving effects. It is greater than 100-fold selective for PDE4A, -B, and -D (IC50s = 2.51, 1.58, and 2 nM for PDE4A, PDE4B, and PDE4D, respectively) over 10 other members of the PDE family, as well as over a panel of 154 diverse receptors, ion channels, and enzymes. It inhibits LPS-induced release of TNF-alpha in isolated human whole blood (IC50 = 23.1 nM) and reduces LPS-induced neutrophilia in rats (ED50 = 0.09 mg/kg). GSK356278 (0.01-1 mg/kg) induces anxiolytic behavior in marmosets, and improves performance of non-human primates in an object retrieval test when administered at a dose of 1 mg/kg.Formal Name: 5-[5-[(2,4-dimethyl-5-thiazolyl)methyl]-1,3,4-oxadiazol-2-yl]-1-ethyl-N-(tetrahydro-2H-pyran-4-yl)-1H-pyrazolo[3,4-b]pyridin-4-amine. CAS Number: 720704-34-7. Molecular Formula: C21H25N7O2S. Formula Weight: 439.5. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: Chloroform: 30 mg/ml. lambdamax: 247, 255, 310 nm. SMILES: CC1=C(CC2=NN=C(C3=CN=C4C(C=NN4CC)=C3NC5CCOCC5)O2)SC(C)=N1. InChi Code: InChI=1S/C21H25N7O2S/c1-4-28-20-15(11-23-28)19(25-14-5-7-29-8-6-14)16(10-22-20)21-27-26-18(30-21)9-17-12(2)24-13(3)31-17/h10-11,14H,4-9H2,1-3H3,(H,22,25). InChi Key: AWDJJMXJUOHGLC-UHFFFAOYSA-N.