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  • KB-R7943 mesylate
    • KB R7943; KB-R 7943, KBR7943, 182004-65-5, KB-R7943 mesylate, 2-[2-[4-(4-NITROBENZYLOXY)PHENYL]ETHYL]ISOTHIOUREA MESYLATE, IN1281, KB-R 7943
    货号: abs810631
    CAS号: 182004-65-5
    分子式: C17H21N3O6S2
    分子量: 427.5
    产品说明书
    分享:
    货号-规格 货期 价格 数量
    abs810631-10mg 1-2周 ¥958.00
    - +
    abs810631-50mg 1-2周 ¥3383.00
    - +
    abs810631-100mg 1-2周 ¥6174.00
    - +
    大包装询价
    产品描述
    描述

    KB-R7943 mesylate is a potent, selective inhibitor of the reverse mode of the Na+/Ca2+ exchanger (IC50 = 0.7 mM).

    纯度
    >98%
    储存/保存方法
    store at -20℃ for one year(Powder);
    in DMSO or others solvent store at 2-4℃ for two weeks, at -80℃ for six months.
    基本信息
    别名
    KB R7943; KB-R 7943, KBR7943, 182004-65-5, KB-R7943 mesylate, 2-[2-[4-(4-NITROBENZYLOXY)PHENYL]ETHYL]ISOTHIOUREA MESYLATE, IN1281, KB-R 7943
    外观
    Powder
    可溶性/溶解性
    DMSO : ≥ 27 mg/mL

    H2O : 4.3 mg/mL (Need warming)
    生物活性
    靶点
    Na(addition)_Ca2(addition) Exchanger
    In vitro(体外研究)
    KB-R7943 mesylate blocks NMDAR-mediated ion currents, and inhibits NMDA-induced increase in cytosolic Ca2+ with IC50=13.4±3.6 µM but accelerates calcium deregulation and mitochondrial depolarization in glutamate-treated neurons. KB-R7943 depolarizes mitochondria in a Ca2+-independent manner. KB-R7943 inhibits 2,4-dinitrophenol-stimulated respiration of cultured neurons with IC50=11.4±2.4 µM. In addition to NCXrev, KB-R7943 dose-dependently and reversibly blocked ion currents elicited by NMDA. KB-R7943 dose-dependently inhibits NMDA-induced increases in c with IC50=13.4±3.6 µM confirming the inhibition of NMDA receptors observed in electrophysiological experiments. wtRyR1-HEK 293 pretreated with KB-R7943 (10 μM, 10 min) dissolved in the bulk perfusion exhibited significantly attenuated responses to caffeine. In this regard, KB-R7943 produced more pronounced inhibition of caffeine-induced Ca2+ release elicited by 1 mM compared with 0.5 and 0.75 mM (60 versus 58 versus 37%, p. KB-R7943 inhibits both IhERG and native IKr rapidly on membrane depolarization with IC50 values of ~89 and ~120 nM, respectively, for current tails at −40 mV following depolarizing voltage commands to +20 mV. IhERG inhibition by KB-R7943 exhibits both time- and voltage-dependence but shows no preference for inactivated over activated channels.
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