A PDE4B inhibitor
货号:ajcx23248
CAS:2410550-31-9
分子式:C17H11Cl2F2N3O
分子量：382.2
溶解度:DMF: 30 mg/ml,DMSO: 30 mg/ml,DMSO:PBS (pH 7.2) (1:5): 0.16 mg/ml
纯度：98%
存储：Store at -20°C
库存：现货

Background:

PDE4B inhibitor is an inhibitor of phosphodiesterase 4B (PDE4B; IC₅₀= 140 nM).^1,2It 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-HT_2C, and sigma-2 (σ₂) receptors by greater than 50%.¹PDE4B inhibitor (1 µM) decreases LPS- or Pam₃Cys-induced production of TNF-α 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.²

1.Vadukoot, A.K., Sharma, S., Aretz, C.D., et al.Synthesis and SAR studies of 1H-pyrrolo[2,3-b]pyridine-2-carboxamides as phosphodiesterase 4B (PDE4B) inhibitorsACS Med. Chem. Lett.11(10)1848-1854(2020) 2.Burkovetskaya, M.E., Liu, Q., Vadukoot, A.K., et al.KVA-D-88, a novel preferable phosphodiesterase 4B inhibitor, decreases cocaine-mediated reward properties in vivoACS Chem. Neurosci.11(15)2231-2242(2020)