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首页-小分子抑制剂&激动剂-GPCR-Melanocortin Receptor-PF-07258669
PF-07258669

Chemical Structure : PF-07258669

CAS No.: 2755890-53-8

PF-07258669 (PF 07258669)

货号: 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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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

    生物&药学活性

    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.

    物理化学性质&存储条件

    分子量 462.53
    分子式 C25H27FN6O2
    外观性状 Solid
    CAS No.
    储存条件
    固体粉末
    -20°C 12 个月; 4°C 6 个月
    配置液
    -80°C 6 个月; -20°C 6 个月
    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

    参考文献

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

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