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首页-小分子抑制剂&激动剂-Membrane Transporter/Ion Channel-iGluR-GNE-9278
GNE-9278

Chemical Structure : GNE-9278

CAS No.: 2315311-83-0

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GNE-9278 (GNE9278)

货号: PC-49066Not For Human Use, Lab Use Only.

GNE-9278 is a potent NMDAR positive allosteric modulator (PAM) that acts at the GluN1 transmembrane domain (TMD), robustly potentiates GluN2A, 2B, 2C and 2D-containing NMDARs in calcium influx assays from HEK cell lines with EC50 values of 0.74, 3.07, 0.47, and 0.32 μM, respectively, and maximum fold potentiation of 5.5, 8.4, 10.2 and 7.9, respectively.

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

    生物&药学活性

    GNE-9278 is a potent NMDAR positive allosteric modulator (PAM) that acts at the GluN1 transmembrane domain (TMD), robustly potentiates GluN2A, 2B, 2C and 2D-containing NMDARs in calcium influx assays from HEK cell lines with EC50 values of 0.74, 3.07, 0.47, and 0.32 μM, respectively, and maximum fold potentiation of 5.5, 8.4, 10.2 and 7.9, respectively.
    GNE-9278 is highly selective for NMDARs vs. AMPARs, with no appreciable activity in AMPAR calcium influx assays.
    GNE-9278 demonstrates robust potentiation of GluN2A, 2B, 2C and 2D-containing NMDARs in electrophysiology experiments in oocytes with EC50 values of 3.2, 15.7, 6.6 and 6.7 μM, respectively, and maximum fold potentiation of 4.6, 12.4, 9.1 and 14.9, respectively.
    Modulation by GNE-9278 is state-dependent and significantly alters extracellular domain pharmacology.

    物理化学性质&存储条件

    分子量 429.539
    分子式 C21H27N5O3S
    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-cyclohexyl-N-(5-methyl-7-oxo-2-propyl-4,7-dihydro-[1,2,4]triazolo[1,5-a]pyrimidin-6-yl)benzenesulfonamide

    参考文献

    1. Tzu-Ming Wang, et al. Neuropharmacology. 2017 Jul 15;121:204-218.

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