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首页-小分子抑制剂&激动剂-Membrane Transporter/Ion Channel-iGluR-GluN2A PAM Y36
GluN2A PAM Y36

Chemical Structure : GluN2A PAM Y36

CAS No.: 3110701-06-6

GluN2A PAM Y36

货号: PC-25186Not For Human Use, Lab Use Only.

GluN2A PAM Y36 is a potent, GluN2A-selective N-Methyl-d-aspartate receptor (NMDAR) positive allosteric modulator with EC50 of 24.97 uM, Emax=397.7%.

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

    生物&药学活性

    GluN2A PAM Y36 is a potent, GluN2A-selective N-Methyl-d-aspartate receptor (NMDAR) positive allosteric modulator with EC50 of 24.97 uM, Emax=397.7%.
    Y36 showed higher efficacy (Emax = 397.7%) than GNE-3419 (Emax = 196.4%), reducing the EC50 values and increasing the Emax values for glutamate/glycine at GluN2A receptor.
    Y36 significantly alleviated depression-related behaviors in multiple behavioral assessments in chronic restraint stress (CRS) mice.
    Y36 has favorable pharmacokinetic (PK) profiles and blood-brain barrier (BBB) penetration, with no signs of addiction, weight gain, or organ and tissue damage in mice.

    物理化学性质&存储条件

    分子量 373.45
    分子式 C19H20FN3O2S
    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

    7-((4-(4-Fluorophenyl)-4-hydroxypiperidin-1-yl)methyl)-2-methyl-5H-thiazolo[3,2-a]pyrimidin-5-one

    参考文献

    1. Tingting Yang, et al. J Med Chem. 2025 Jul 31. doi: 10.1021/acs.jmedchem.5c01173.

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