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KB-R7943
KB-R7943
KB-R7943
商品货号:MB3481
CAS 号:182004-65-5
英文名字:KB R7943 mesylate
质量标准:>98%,BR
分子式:C17H21N3O6S2
  • 包装规格:
    规格 库存 发货时间
    10MG [¥750.00]15 现货
    50MG [¥2380.00]15 现货
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    商品信息

    质检证书(coa)

    说明书下载

    KB-R7943
    KB-R7943 mesylate 是一种 Na+/Ca2+ 交换体 (NCXrev) 反向抑制剂,IC50 为 5.7±2.1 µM。
    分子量:427.5;分子式:C17H21N3O6S2

    相关谱图:

    HNMR
    生物活性:

    Description

    KB-R7943 mesylate is a widely used inhibitor of the reverse Na+/Ca2+ exchanger (NCXrev) with IC50 of 5.7±2.1 µM.

    IC50 & Target

    IC50: 5.7±2.1 µM (Na+/Ca2+ exchanger)

    In Vitro

    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 [Ca2+]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<0.05, respectively). 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

    实验操作(仅供参考)

    储液制备

    Concentration/ Volume (DMSO) /Mass

    1 mg

    5 mg

    10 mg

    1 mM

    2.3392 mL

    11.6959 mL

    23.3918 mL

    5 mM

    0.4678 mL

    2.3392 mL

    4.6784 mL

    10 mM

    0.2339 mL

    1.1696 mL

    2.3392 mL

    Cell Assay

    KB-R7943 mesylate is dissolved in DMSO and stored, and then diluted with appropriate medium before use.
    EK 293 cells stably expressing the wtRyR1 (wtRyR1-HEK 293) are maintained in Dulbecco's modified Eagle's medium supplemented with 2 mM glutamine, 100 μg/mL streptomycin, 100 U/mL penicillin, 1 mM sodium pyruvate, and 10% fetal bovine serum at 37°C under 5% CO2. wtRyR1-HEK 293 cells are loaded with 5 μM Fluo-4 acetoxymethyl ester at 37°C for 30 min to measure Ca2+ transients in an imaging buffer consisting of 140 mM NaCl, 5 mM KCl, 2 mM MgCl2, 2 mM CaCl2, 10 mM HEPES, and 10 mM glucose, pH 7.4, supplemented with 0.05% bovine serum albumin. The cells are washed three times with imaging buffer and additionally incubated for 20 min at room temperature. Dye-loaded cells are washed three times with imaging buffer and imaged with a charge-coupled device camera with a 40× objective lens attached to an IX-71 microscope. The sequence of images is captured and monitored using EasyRatioPro. Caffeine dissolved in the imaging buffer is focally applied for 15 s using AutoMate Scientific. KB-R7943 is dissolved in the imaging buffer, and wtRyR1-HEK 293 cells are incubated for 10 min before the application of caffeine. They are for reference only.

    溶解性:DMSO: ≥ 20 mg/mL; H2O:3 mg/mL (Need warming)
    储存条件:-20°C

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