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NKTR-181

Chemical Structure : NKTR-181

CAS No.: 1211231-76-3

NKTR-181 (NKTR 181;NKTR181;Loxicodegol)

Catalog No.: PC-60802Not For Human Use, Lab Use Only.

A novel, long-acting and orally active, selective mu-opioid agonist that displays higher binding affinity (Ki=237 nM) at the MOR than kappa and delta opioid receptors (>100-fold).

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    Biological Activity

    NKTR-181 (Loxicodegol) is a long-acting and orally active, selective mu-opioid agonist that displays higher binding affinity (Ki=237 nM) at the MOR than kappa and delta opioid receptors (>100-fold);.
    NKTR-181 demonstrates maximum analgesic activity comparable to that of oxycodone in hot-plate latency and acetic-acid writhing models.
    NKTR-181 reduces its rate of entry across the blood-brain barrier compared with traditional mu-opioid agonists.

    Physicochemical Properties

    M.Wt 595.73
    Formula C31H49NO10
    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

    (4R,4aS,7S,7aR,12bS)-7-((2,5,8,11,14,17-hexaoxanonadecan-19-yl)oxy)-9-methoxy-3-methyl-1,2,3,4,5,6,7,7a-octahydro-4aH-4,12-methanobenzofuro[3,2-e]isoquinolin-4a-ol

    References

    1. Miyazaki T, et al. J Pharmacol Exp Ther. 2017 Oct;363(1):104-113.

    2. Webster L, et al. Pain Med. 2017 Mar 10. doi: 10.1093/pm/pnw344.

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