Product Data SheetProduct Name:CAS No.: Cat. No.:MWt:Formula:Purity :PF-25459208562-94-2HY-50098392.45C25H20N4O>98%Solubility:DMSOMechanisms: Pathways:Others ; Target:PDE gyBiological Activity:PF-2545920 a highly selective and potent PDE10A inhibitor with an IC50 of 0.37 nM. The PDE10Aenzyme is expressed primarily in the brain, mostly in the striatum, nucleus accumbens and olfactorytubercle, and is thought to be particularly important in regulating the activity of dopamine-sensitivemedium spiny neurons in the striatum which are known to be targets of conventional antipsychoticagents. n the conditioned avoidance response assay (CAR), PF-2545920 was active with an ED50of 1 mg/kg. Administration of PF-2545920 to mice caused a dose dependent increase in striatalcGMP.References:[1]. Verhoest PR et al. Discovery of a novel class of phosphodiesterase 10A inhibitors andidentification of clinical candidate 2-[4-(1-methyl-4-pyridin-4-yl-1H-pyrazol-3-yl)-phenoxymethyl]-quinoline (PF-2545920) for the treatment of schizophrenia. J Med Chem [][2]. Verhoest PR, Chapin DS, Corman M, Fonseca K, Harms JF, Hou X, Marr ES, Menniti FS,pNelson F, O'Connor R, Pandit J, Proulx-Lafrance C, Schmidt AW, Schmidt CJ, Suiciak JA, LirasS.,Discovery of a novel class of phosphodiesterase 10A inhibitors and identification of clinicalcandidate 2-[4-(1-methyl-4-pyridin-4-yl-1H-pyrazol-3-yl)-phenoxymethyl]-quinoline (PF-2545920) forthe treatment of schizophrenia.,J Med Chem. 2009 Aug 27;52(16):5188-96. [3]. Hu E, Ma J, Biorn C, Lester-Zeiner D, Cho R, Rumfelt S, Kunz RK, Nixey T, Michelsen K, MillerS, Shi J, Wong J, Hill Della Puppa G, Able J, Talreja S, ...Caution: Not fully tested. For research purposes onlyMedchemexpress LLCwww.medchemexpress.com 18 Wilkinson Way, Princeton, NJ 08540,USAEmail: info@medchemexpress.com Web: www.medchemexpress.com
