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首页-小分子抑制剂&激动剂-GPCR-Histamine Receptor-PF-03654746
PF-03654746

Chemical Structure : PF-03654746

CAS No.: 935840-31-6

PF-03654746 (PF-3654746, PF03654746)

货号: PC-63034Not For Human Use, Lab Use Only.

PF-03654746 (PF-3654746) is a potent, selective, orally bioactive antagonist of H3 receptor with Ki of 2.3 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-03654746 (PF-3654746) is a potent, selective, orally bioactive antagonist of H3 receptor with Ki of 2.3 nM.
    PF-03654746 dislaplays >1000-fold selectivity versus H1, H2, H4 and other GPCRs (IC50>10 uM).
    PF-03654746 possesses optimal pharmacological and pharmacokinetic profiles, shows potential in allergen-induced nasal symptoms.

    物理化学性质&存储条件

    分子量 322.4
    分子式 C18H24F2N2O
    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

    Trans-N-ethyl-3-fluoro-3-[3-fluoro-4-(pyrrolidinylmethyl)phenyl]cyclobutanecarboxamide

    参考文献

    1. Wager TT, et al. J Med Chem. 2011 Nov 10;54(21):7602-20.

    2. Stokes JR, et al. J Allergy Clin Immunol. 2012 Feb;129(2):409-12, 412.e1-2.

    3. Gallezot JD, et al. J Cereb Blood Flow Metab. 2017 Mar;37(3):1095-1107.

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