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首页-小分子抑制剂&激动剂-Epigenetics-HDAC-trans CM-414
trans CM-414

Chemical Structure : trans CM-414

CAS No.: 1624792-73-9

trans CM-414 (CM 414;CM414)

货号: PC-60416Not For Human Use, Lab Use Only.

trans CM-414 is a first-in-class, dual inhibitor of PDE5 and HDAC that inhibits HDAC1/2/3/6 (IC50=310/490/322/91 nM, respectively) and PDE5 (IC50=60 nM).

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

    生物&药学活性

    trans CM-414 is a first-in-class, dual inhibitor of PDE5 and HDAC that inhibits HDAC1/2/3/6 (IC50=310/490/322/91 nM, respectively) and PDE5 (IC50=60 nM).
    trans CM-414 does not inhibit class IIa HDAC isoforms, MMP-3, MMP-10, and PDE9 (IC50>10 uM), has modest or weak activity for HDAC8/11/10 (IC50=640/550/2400 nM).
    trans CM-414 diminishes brain Aβ and pTau levels, increases the inactive form of GSK3β, reverts the decrease in dendritic spine density on hippocampal neurons, and reverses the cognitive deficits in Tg2576 mice.

    物理化学性质&存储条件

    分子量 439.516
    分子式 C23H29N5O4
    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

    3-(4-ethoxy-3-(1-methyl-7-oxo-3-propyl-6,7-dihydro-1H-pyrazolo[4,3-d]pyrimidin-5-yl)benzyl)-N-hydroxycyclobutane-1-carboxamide​, trans-

    参考文献

    1. Cuadrado-Tejedor M, et al. Neuropsychopharmacology. 2017 Jan;42(2):524-539.

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