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首页-小分子抑制剂&激动剂-Membrane Transporter/Ion Channel-Calcium Channel -HSK16149
HSK16149

Chemical Structure : HSK16149

CAS No.: 2209104-84-5

HSK16149 (Crisugabalin, HSK 16149)

货号: PC-49748Not For Human Use, Lab Use Only.

HSK16149 (Crisugabalin) is a potent selective ligand of voltage-gated calcium channel (VGCC) α2δ subunit with IC50 of 3.96 nM in competitive [3H]gabapentin binding assays.

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

    生物&药学活性

    HSK16149 (Crisugabalin) is a potent selective ligand of voltage-gated calcium channel (VGCC) α2δ subunit with IC50 of 3.96 nM in competitive [3H]gabapentin binding assays.
    HSK16149 exhibited stronger (>20-fold) affinity than pregabalin.
    In rat models of neuropathic pain, the minimum effective dose (MED) of HSK16149 was 10 mg/kg, and the efficacy was similar to that of 30 mg/kg pregabalin.
    HSK16149 could persist up to 24 hours postadministration at 30 mg/kg, whereas the efficacy of pregabalin lasted only for 12 hours at 30 mg/kg in streptozotocin-induced diabetic neuropathy model.
    HSK16149 also inhibit mechanical allodynia in intermittent cold stress model and decrease phase II pain behaviors in formalin-induced nociception model.

    物理化学性质&存储条件

    分子量 209.29
    分子式 C12H19NO2
    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

    2-((1S,2S,3R,6S,8S)-2-(aminomethyl)tricyclo[4.2.1.03,8]nonan-2-yl)acetic acid

    参考文献

    1. Xiaoli Gou , et al. J Pharmacol Exp Ther. 2021 Mar;376(3):330-337.

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