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PF-04455242 hydrochloride

CAS No. 1322001-35-3

PF-04455242 hydrochloride( PF-4455242 )

Catalog No. M11299 CAS No. 1322001-35-3

PF-04455242 is a potent, selective κ-opioid receptor (KOR) antagonist with Ki of 3 nM/21 nM/22 nM for hKOR/rKOR/mKOR, respectively.

Purity : >98% (HPLC)

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Biological Information

  • Product Name
    PF-04455242 hydrochloride
  • Note
    Research use only, not for human use.
  • Brief Description
    PF-04455242 is a potent, selective κ-opioid receptor (KOR) antagonist with Ki of 3 nM/21 nM/22 nM for hKOR/rKOR/mKOR, respectively.
  • Description
    PF-04455242 is a potent, selective κ-opioid receptor (KOR) antagonist with Ki of 3 nM/21 nM/22 nM for hKOR/rKOR/mKOR, respectively; shows 20-fold reduced affinity for hMOR and negligible affinity for DOR (Ki>4 uM); demonstrates antidepressant-like efficacy, attenuates the behavioral effects of stress, dose-dependently reduceds the elevation of spiradoline-induced plasma prolactin in rats.Depression Phase 1 Discontinued.
  • In Vitro
    ——
  • In Vivo
    ——
  • Synonyms
    PF-4455242
  • Pathway
    Endocrinology/Hormones
  • Target
    Opioid Receptor
  • Recptor
    Opioid Receptor
  • Research Area
    Neurological Disease
  • Indication
    Depression

Chemical Information

  • CAS Number
    1322001-35-3
  • Formula Weight
    408.985
  • Molecular Formula
    C21H29ClN2O2S
  • Purity
    >98% (HPLC)
  • Solubility
    ——
  • SMILES
    O=S(C1=CC=CC=C1C2=CC=C(CNCC(C)C)C=C2)(N3CCCC3)=O.[H]Cl
  • Chemical Name
    2-Methyl-N-[[4-(2-pyrrolidin-1-ylsulfonylphenyl)phenyl]methyl]propan-1-amine hydrochloride

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1. Verhoest PR, et al. J Med Chem. 2011 Aug 25;54(16):5868-77. 2. Grimwood S, et al. J Pharmacol Exp Ther. 2011 Nov;339(2):555-66. 3. Melief EJ, et al. Mol Pharmacol. 2011 Nov;80(5):920-9.
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