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Rexaceract

Chemical Structure : Rexaceract

CAS No.: 2648407-86-5

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Rexaceract (GT-02287, GT02287)

货号: PC-26353Not For Human Use, Lab Use Only.

Rexaceract (GT-02287) is a potent, selective positive allosteric modulator (PAM) of beta-glucocerebrosidase (β-glucocerebrosidase, β-glucosidase, or GCase) with KD of 17-24 uM at pH 7.4, enhances the function of lysosomal GCase.

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

    生物&药学活性

    Rexaceract (GT-02287) is a potent, selective positive allosteric modulator (PAM) of beta-glucocerebrosidase (β-glucocerebrosidase, β-glucosidase, or GCase) with KD of 17-24 uM at pH 7.4, enhances the function of lysosomal GCase.
    Rexaceract (GT-02287) enhances GCase activity and facilitates its transport to lysosomes.
    Rexaceract (GT-02287) increases GCase activity in fibroblast lysates by binding to a site distinct from the active site.
    Rexaceract (GT-02287) (1.56-12.5 uM) effectively reduced GlcCer levels in patient fibroblasts.
    Rexaceract (GT-02287) promotes lysosomal delivery of the ER-retained variant GCaseLeu444Pro, promotes CNX release and prevent proteasomal degradation of GCaseLeu444Pro.
    Rexaceract (GT-02287) alleviates UPR in p.N370S/ins and p.L444P/p.L444P patient fibroblasts.

    物理化学性质&存储条件

    分子量 362.41
    分子式 C21H19FN4O
    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-amino-N-(2,3-dihydro-1H-inden-2-yl)-6-((2-fluorophenyl)amino)picolinamide

    参考文献

    1. Patent WO2021105908 A1 2021-06-03. 2. Fregno I, et al. Int J Mol Sci. 2025 May 6;26(9):4392.

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