PDE4B Inhibitor

PDE4B inhibitor is an inhibitor of phosphodiesterase 4B (PDE4B, IC50 = 140 nM). It is selective for PDE4B over a panel of 20 PDE isoforms and a panel of 39 CNS receptors at 10 µM but does inhibit the activity of PDE4C1, PDE3B, the serotonin (5-HT) receptor subtype 5-HT2C, and sigma-2 (sigma2) receptors by greater than 50%. PDE4B inhibitor (1 µM) decreases LPS- or Pam3Cys-induced production of TNF-alpha in mouse bone marrow-derived macrophages (BMDMs). It reduces cocaine self-administration and the progressive ratio breakpoint in mice when administered at a dose of 5 mg/kg.Formal Name: [1-(3,4-dichlorophenyl)-1H-pyrrolo[2,3-b]pyridin-2-yl](3,3-difluoro-1-azetidinyl)-methanone. CAS Number: 2410550-31-9. Synonyms: KVA-D-88. Molecular Formula: C17H11Cl2F2N3O. Formula Weight: 382.2. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMSO: 30 mg/ml, DMSO:PBS (pH 7.2) (1:5): 0.16 mg/ml. lambdamax: 298 nm. SMILES: O=C(N1CC(F)(C1)F)C2=CC3=C(N2C4=CC=C(C(Cl)=C4)Cl)N=CC=C3. InChi Code: InChI=1S/C17H11Cl2F2N3O/c18-12-4-3-11(7-13(12)19)24-14(6-10-2-1-5-22-15(10)24)16(25)23-8-17(20,21)9-23/h1-7H,8-9H2. InChi Key: JQEUSIGJVMRCOL-UHFFFAOYSA-N.