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PF-07258669

Chemical Structure : PF-07258669

CAS No.: 2755890-53-8

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PF-07258669 (PF 07258669)

Catalog No.: PC-49760Not For Human Use, Lab Use Only.

PF-07258669 (PF 07258669) is a potent, selective, and orally bioavailable melanocortin-4 receptor (MC4R) antagonist with Ki of 0.46 nM and human MC4R inverse agonist potency (IC50=13 nM).

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

    Biological Activity

    PF-07258669 (PF 07258669) is a potent, selective, and orally bioavailable melanocortin-4 receptor (MC4R) antagonist with Ki of 0.46 nM and human MC4R inverse agonist potency (IC50=13 nM).
    PF-07258669 weakly binds hMC3R, hMC5R and hMC1R with Ki values of 340 nM, 840 nM, and >1600 nM, respectively.
    PF-07258669 showed robust in vivo efficacy in an aged rat in vivo model of geriatric anorexia.

    Physicochemical Properties

    M.Wt 462.53
    Formula C25H27FN6O2
    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

    (2R)-2-(5-Fluoro-2-methoxypyridin-4-yl)-1-[(2S)-7-methyl-6-(pyrimidin-2-yl)-3,4-dihydro-1H-spiro[1,8-naphthyridine-2,3'-pyrrolidin]-1'-yl]propan-1-one

    References

    1. Michelle R Garnsey, et al. J Med Chem. 2023 Feb 19. doi: 10.1021/acs.jmedchem.2c02012.

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