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首页-小分子抑制剂&激动剂-Membrane Transporter/Ion Channel-Calcium Channel -TROX-1
TROX-1

Chemical Structure : TROX-1

CAS No.: 1309601-26-0

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TROX-1 (TROX 1, TROX1)

货号: PC-60679Not For Human Use, Lab Use Only.

TROX-1 is a potent, state-dependent blocker of Cav2 channels that preferentially inhibits potassium-triggered calcium influx through recombinant Cav2.2 under depolarized conditions with IC50 of 0.27 uM, compared with hyperpolarized conditions (IC50>20 uM).

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

    生物&药学活性

    TROX-1 is a potent, state-dependent blocker of Cav2 channels that preferentially inhibits potassium-triggered calcium influx through recombinant Cav2.2 under depolarized conditions with IC50 of 0.27 uM, compared with hyperpolarized conditions (IC50>20 uM).
    TROX-1 inhibits omiga-conotoxin GVIA-sensitive calcium currents with greater potency under depolarized conditions (IC50=0.4 uM) in rat DRG neurons, blocks all Ca(v)2 family channels.
    TROX-1 reduces nociception in preclinical pain models, while sparing normal cardiac and behavioral functions.

    物理化学性质&存储条件

    分子量 434.859
    分子式 C22H16ClFN6O
    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

    (3R)-5-(3-chloro-4-fluorophenyl)-3-methyl-3-(pyrimidin-5-ylmethyl)-1-(1H-1,2,4-triazol-3-yl)-1,3-dihydro-2H-indol-2-one

    参考文献

    1. Abbadie C, et al. J Pharmacol Exp Ther. 2010 Aug;334(2):545-55.

    2. Swensen AM, et al. Mol Pharmacol. 2012 Mar;81(3):488-97.

    3. Patel R, et al. Neuroscience. 2015 Jun 25;297:47-57.

    4. Rahman W, et al. Neuroscience. 2015 Oct 1;305:76-85.

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