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首页-小分子抑制剂&激动剂-Metabolic Enzyme/Protease-Phosphodiesterase (PDE)-RF26
RF26

Chemical Structure : RF26

CAS No.: 2699052-46-3

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RF26 (Compound d12)

货号: PC-23406Not For Human Use, Lab Use Only.

RF26 (Compound d12) is a highly potent and selective PDE5 inhibitor with IC50 of 1 nM, three times more potent than sildenafil and more selective with a selectivity index of >10,000-fold against all other PDE isozymes.

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

    生物&药学活性

    RF26 (Compound d12) is a highly potent and selective PDE5 inhibitor with IC50 of 1 nM, three times more potent than sildenafil and more selective with a selectivity index of >10,000-fold against all other PDE isozymes.
    RF26 has a mechanism of enzyme inhibition distinct from sildenafil.
    RF26 is active against PDE5 catalytic domain (IC50=1 nM, full-length PDE5), but not PDE5 catalytic domain even at 1 uM.
    RF26 inhibits PDE5 and increase the intracellular cGMP in live HEK-293 cells transfected to stably express a cGMP biosensor (EC50=6.7 uM).
    RF26 improves memory impairment and ameliorates tau aggregation and neuroinflammation in the P301S tauopathy mouse model of Alzheimer's disease.

    物理化学性质&存储条件

    分子量 470.56
    分子式 C26H32F2N4O2
    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

    (4-(3-(tert-Butyl)-5-(3,5-difluoro-4-methoxyphenyl)-4,5-dihydro-1H-pyrazol-1-yl)phenyl)(4-methylpiperazin-1-yl)methanone

    参考文献

    1. Sigler S, et al. Anticancer Agents Med Chem. 2024 Sep 2. doi: 10.2174/0118715206318802240821114353.

    2. El-Desouky S, et al. Exp Neurol. 2024 Nov 14:115058.

    3. Abdel-Halim M, et al. J Med Chem. 2021 Apr 22;64(8):4462-4477.

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