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BMS-470539

Chemical Structure : BMS-470539

CAS No.: 2341796-82-3

BMS-470539 (BMS 470539;BMS470539)

Catalog No.: PC-60215Not For Human Use, Lab Use Only.

BMS-470539 is a potent, selective, full agonist of human and murine melanocortin-1 receptor (MC-1R) with EC50 of 16.8 and 11.6 nM, respectively.

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    Biological Activity

    BMS-470539 is a  potent, selective, full agonist of human and murine melanocortin-1 receptor (MC-1R) with EC50 of 16.8 and 11.6 nM, respectively.
    BMS-470539 dose-dependently inhibits TNFα-induced activation of a NF-kappaB transcriptional reporter in human melanoma cells.
    BMS-470539 inhibits LPS-induced TNFα production in BALB/c mice (EC50=10 uM/kg).
    BMS-470539 inhibits leucocyte trafficking in the inflamed vasculature.

    Physicochemical Properties

    M.Wt 632.63
    Formula C32H43Cl2N5O4
    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

    (S)-2-amino-N-((R)-1-(4-butyryl-4-phenylpiperidin-1-yl)-3-(4-methoxyphenyl)-1-oxopropan-2-yl)-3-(1-methyl-1H-imidazol-5-yl)propanamide dihydrochloride

    References

    1. Kang L, et al. J Leukoc Biol. 2006 Oct;80(4):897-904.

    2. Leoni G, et al. Br J Pharmacol. 2010 May;160(1):171-80.

    3. Doyle JR, et al. J Pharmacol Exp Ther. 2012 Aug;342(2):318-26.

    4. Herpin TF, et al. J Med Chem. 2003 Mar 27;46(7):1123-6.

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