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首页-小分子抑制剂&激动剂-GPCR-Sigma Receptor-FEM-1689
FEM-1689

Chemical Structure : FEM-1689

CAS No.: 2113664-14-3

FEM-1689 (FEM1689)

货号: PC-20739Not For Human Use, Lab Use Only.

FEM-1689 (FEM1689) is a potent, selective σ2R/TMEM97 binding ligand with Ki value of 11 nM.

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

    生物&药学活性

    FEM-1689 (FEM1689) is a potent, selective σ2R/TMEM97 binding ligand with Ki value of 11 nM.
    FEM-1689 is >100-fold more selective for σ2R/TMEM97 than 40 CNS proteins except for σ1R (19-fold) and norepinephrine transporter (NET; 37-fold).
    FEM-1689 inhibits the integrated stress response and promotes neurite outgrowth via a σ2R/TMEM97-specific action in primary mouse dorsal root ganglion (DRG) neurons.
    FEM-1689 reduces ISR and p-eIF2α levels in human sensory neurons and alleviates the pathogenic engagement of integrated stress response (ISR) by methylglyoxal.
    FEM-1689 (10 mg/kg, i.v.) produced analgesic effect in mouse neuropathic pain models.

    物理化学性质&存储条件

    分子量 361.41
    分子式 C21H22F3NO
    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-(8-(4-(trifluoromethyl)phenyl)-1,3,4,5-tetrahydro-2H-1,5-methanobenzo[c]azepin-2-yl)propan-1-ol

    参考文献

    1. Yousuf MS, et al. bioRxiv. 2023 Apr 11:2023.04.11.536439.

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