PF-2545920

CHF 60.00
In stock
AG-CR1-3636-M0011 mgCHF 60.00
AG-CR1-3636-M0055 mgCHF 180.00
AG-CR1-3636-M02525 mgCHF 540.00
 
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Product Details
Synonyms 2-(4-(1-Methyl-4-(pyridin-4-yl)-1H-pyrazol-3-yl)-phenoxymethyl)quinoline; MP-10
Product Type Chemical
Properties
Formula C25H20N4O
MW 392.5
CAS 898562-94-2
Purity Chemicals ≥98% (HPLC)
Appearance Solid.
Solubility Soluble in DMSO or ethanol. Insoluble in water.
Identity Determined by 1H-NMR.
InChi Key AZEXWHKOMMASPA-UHFFFAOYSA-N
Shipping and Handling
Shipping AMBIENT
Short Term Storage +4°C
Long Term Storage -20°C
Handling Advice Keep cool and dry.
Use/Stability Stable for at least 2 years after receipt when stored at -20°C.
Store solutions at -20°C in the dark.
Documents
MSDS Download PDF
Product Specification Sheet
Datasheet Download PDF
  • 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).
Product References
  1. 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)
  2. 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)
  3. Effects of phosphodiesterase 10 inhibition on striatal cyclic AMP and peripheral physiology in rats: A. Torremans, et al.; Acta Neurobiol. Exp. 70, 13 (2010)
  4. 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)
  5. β-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)
  6. A novel thermoregulatory role for PDE10A in mouse and human adipocytes: M.K. Hankir, et al.; EMBO Mol. Med. 8, 796 (2016)
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