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PN6047

Chemical Structure : PN6047

CAS No.: 1948274-13-2

PN6047 (PN 6047)

Catalog No.: PC-49002Not For Human Use, Lab Use Only.

PN6047 is an orally bioavailable, G protein-biased and selective δ opioid agonist with pKi of 7.25, fully engages G protein signaling but is a partial agonist in both the arrestin recruitment and internalization assays.

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    Biological Activity

    PN6047 is an orally bioavailable, G protein-biased and selective δ opioid agonist with pKi of 7.25, fully engages G protein signaling but is a partial agonist in both the arrestin recruitment and internalization assays.
    PN6047 elicited a concentration-dependent activation of Gαi G proteins in cells expressing the human δ opioid receptor with EC50 of 13.5 nM, with no effect on Gαi activation in cells expressing either the rat µ opioid receptor or human κ opioid receptors.
    PN6047 (1, 3, 10 mg/kg, p.o.) is an effective antihyperalgesic in the mouse MIA model of osteoarthritis but not in the carrageenan model of acute inflammatory pain.
    PN6047 does not appear to have proconvulsive activity or induce analgesic tolerance.

    Physicochemical Properties

    M.Wt 460.596
    Formula C26H28N4O2S
    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

    3-[[4-(dimethylcarbamoyl)phenyl]-[1-(thiazol-5-ylmethyl)-4-piperidylidene]methyl]benzamide

    References

    1. Alexandra E Conibear, et al. J Pharmacol Exp Ther. 2020 Feb;372(2):224-236.

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