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PF-04455242

Chemical Structure : PF-04455242

CAS No.: 1202647-54-8

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PF-04455242 (PF-4455242, PF 04455242)

Catalog No.: PC-62108Not For Human Use, Lab Use Only.

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.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

    Biological Activity

    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.
    PF-04455242 shows 20-fold reduced affinity for hMOR and negligible affinity for DOR (Ki>4 uM).
    PF-04455242 demonstrates antidepressant-like efficacy, attenuates the behavioral effects of stress, dose-dependently reduceds the elevation of spiradoline-induced plasma prolactin in rats.

    Physicochemical Properties

    M.Wt 372.527
    Formula C21H28N2O2S
    Appearance Solid
    CAS No.
    Storage
    Solide Powder
    -20 °C 12 Months; 4°C 6 Months
    In Solvent
    -80 °C 6 Months; -20°C 6 Months
    Shipping
    Solubility

    10 mM in DMSO
    Chemical Name/SMILES

    2-Methyl-N-[[4-(2-pyrrolidin-1-ylsulfonylphenyl)phenyl]methyl]propan-1-amine

    References

    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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