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ProductsBack/PF-2545920 [898562-94-2]
Chemical Structure
Chemical Structure
Chemical Structure

PF-2545920 [898562-94-2]

Research Use Only
AG-CR1-3636
AdipoGen Life Sciences
CAS Number898562-94-2
DownloadMSDS
Product group Chemicals
Estimated Purity>98%
Molecular Weight392.5
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Overview

  • Supplier
    AdipoGen Life Sciences
  • Product Name
    PF-2545920
  • Delivery Days Customer
    10
  • CAS Number
    898562-94-2
  • Certification
    Research Use Only
  • Estimated Purity
    >98%
  • Hazard Information
    Warning
  • Molecular Formula
    C25H20N4O
  • Molecular Weight
    392.5
  • Scientific Description
    Chemical. CAS: 898562-94-2. Formula: C25H20N4O. MW: 392.5. Potent and selective phosphodiesterase 10A (PDE10A) inhibitor (IC50=1.26nM) in vitro and in vivo. PDE10A is a cGMP and cAMP degrading PDE isozyme with neurological importance and was shown to be implicated in the regulation of energy homeostasis. Inhibition of PDE10A leads to interference of the breakdown of the secondary messenger cAMP and cGMP. Anti-psychotic agent. Useful for the treatment of schizophrenia. Anticancer agent. Inhibits colon tumor cell growth for which high levels of PDE10A have been reported. Antiobesity and antidiabetic agent. Induces browning in white adipose tissue (WAT). - Potent and selective phosphodiesterase 10A (PDE10A) inhibitor (IC50=1.26nM) in vitro and in vivo. PDE10A is a cGMP and cAMP degrading PDE isozyme with neurological importance and was shown to be implicated in the regulation of energy homeostasis. Inhibition of PDE10A leads to interference of the breakdown of the secondary messenger cAMP and cGMP. Anti-psychotic agent. Useful for the treatment of schizophrenia. Anticancer agent. Inhibits colon tumor cell growth for which high levels of PDE10A have been reported. Antiobesity and antidiabetic agent. Induces browning in white adipose tissue (WAT).
  • SMILES
    CN(C=C1C2=CC=NC=C2)N=C1C(C=C3)=CC=C3OCC4=NC5=CC=CC=C5C=C4
  • Storage Instruction
    -20°C,2°C to 8°C
  • UNSPSC
    12352200

References

  • Discovery of a novel class of phosphodiesterase 10A inhibitors and identification of clinical candidate 2-[4-(1-methyl-4-pyridin-4-yl-1H-pyrazol-3-yl)-phenoxymethyl]-quinoline (PF-2545920) for the treatment of schizophrenia: P.R. Verhoest, et al.; J. Med. Chem. 52, 5188 (2009)
  • Phosphodiesterase 10A inhibitor activity in preclinical models of the positive, cognitive, and negative symptoms of schizophrenia: S.M. Grauer, et al.; J. Pharmacol. Exp. Ther. 331, 574 (2009)
  • Effects of phosphodiesterase 10 inhibition on striatal cyclic AMP and peripheral physiology in rats: A. Torremans, et al.; Acta Neurobiol. Exp. 70, 13 (2010)
  • Phosphodiesterase 10A inhibitor, MP-10 (PF-2545920), produces greater induction of c-Fos in dopamine D2 neurons than in D1 neurons in the neostriatum: J.M. Wilson, et al.; Neuropharmacol. 99, 379 (2015)
  • beta-catenin nuclear translocation in colorectal cancer cells is suppressed by PDE10A inhibition, cGMP elevation, and activation of PKG: K. Lee, et al.; Oncotarget 7, 5353 (2016)
  • A novel thermoregulatory role for PDE10A in mouse and human adipocytes: M.K. Hankir, et al.; EMBO Mol. Med. 8, 796 (2016)