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首页-小分子抑制剂&激动剂-Membrane Transporter/Ion Channel-Monoamine Transporter-Vanoxerine
Vanoxerine

Chemical Structure : Vanoxerine

CAS No.: 67469-69-6

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Vanoxerine (Boxeprazine, GBR-12909, GBR12909, I893, I-893)

货号: PC-43400Not For Human Use, Lab Use Only.

Vanoxerine (GBR-12909, I-893, Boxeprazine) is a highly potent inhibitor of dopamine uptake in vitro in tissue slices obtained from rat neostriatum with IC50 of 40-50 nM, also inhibits norepinephrine uptake with IC50 of 560-2600 nM.

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

    生物&药学活性

    Vanoxerine (GBR-12909, I-893, Boxeprazine) is a highly potent inhibitor of dopamine uptake in vitro in tissue slices obtained from rat neostriatum with IC50 of 40-50 nM, also inhibits norepinephrine uptake with IC50 of 560-2600 nM.
    Vanoxerine also is a potent hK(v)11.1 blocker, and at submicromolar concentrations.
    Vanoxerine blocks Ca and Na currents in a strongly frequency-dependent manner possesses anticonvulsant activity in zebrafish and rodent models of generalized epilepsy but with cardiac ion channel effects.
    Vanoxerine also is a cancer-specific downregulator of G9a expression, suppresses cancer stem cell functions in colon tumors.

    物理化学性质&存储条件

    分子量 450.5633
    分子式 C28H32F2N2O
    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

    Piperazine, 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)-

    参考文献

    1. Teicher MH, et al. Brain Res. 1986 Nov;395(1):124-8.

    2. Heikkila RE, et al. Eur J Pharmacol. 1984 Aug 17;103(3-4):241-8.

    3. Lacerda AE, et al. J Cardiovasc Electrophysiol. 2010 Mar;21(3):301-10.

    4. Goldsmith P, et al. Pharmacology. 2007;79(4):250-8.

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