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You are here:Home-Chemical Inhibitors & Agonists-GPCR-Melanocortin Receptor-PF-00446687
PF-00446687

Chemical Structure : PF-00446687

CAS No.: 862281-92-3

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PF-00446687 (PF-446687;PF00446687)

Catalog No.: PC-60214Not For Human Use, Lab Use Only.

PF-00446687 (PF-446687) is a potent, selective melanocortin-4 receptor (MC4R) agonist with EC50 of 12 nM.

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

    Biological Activity

    PF-00446687 (PF-446687) is a potent, selective melanocortin-4 receptor (MC4R) agonist with EC50 of 12 nM; displays >100-fold selectivity over MC1R/1 uM); is find to be active in preliminary human trials, with the 200mg dose being of similar effectiveness to 100mg sildenafil, though lower doses were ineffective.

    Sexual Dysfunction

    Phase 2 Clinical

     

    Physicochemical Properties

    M.Wt 470.593
    Formula C28H36F2N2O2
    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

    [(3S,4R)-1-tert-butyl-4-(2,4-difluorophenyl)pyrrolidin-3-yl]-[(3S,5R)-4-hydroxy-3,5-dimethyl-4-phenylpiperidin-1-yl]methanone

    References

    1. Lansdell MI, et al. J Med Chem. 2010 Apr 22;53(8):3183-97.

    2. Modi ME, et al. Neuropsychopharmacology. 2015 Jul;40(8):1856-65.

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