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KB-R7943  99.2165%(HPLC)

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包装规格：10mg 50mg in glass bottle
溶解性：溶于DMSO(>10mg/mL )。
产品描述：基本信息 产品编号： K10014 产品名称： KB-R7943 CAS: 182004-65-5   储存条件 粉末 -20℃ 四年     分子式： C16H17N3O3S.CH3SO3H 溶于液体 -80℃ 6个月 分子量： 427.50 -20℃ 1个月 化学名：  2-[4-[(4-nitrophenyl)methoxy]phenyl]ethyl ester,methanesulfonate (1:1),Carbamimidothioic acid Solubility (25°C)：   体外:   DMSO 86mg/mL (201.16mM) Ethanol Insoluble Water Insoluble 体内(现配现用):   ＜1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。   制备储备液   浓度   溶液体积 质量   1mg   5mg   10mg 1mM 2.3392mL 11.6959mL 23.3918mL 5mM 0.4678mL 2.3392mL 4.6784mL 10mM 0.2339mL 1.1696mL 2.3392mL   生物活性 产品描述 KB-R7943 mesylate是一种Na+/Ca2+交换体 (NCXrev)反向抑制剂，IC50为 5.7±2.1µM。KB-R7943 mesylate通过激活JNK通路和抑制自噬通量来诱导癌细胞死亡. 靶点 IC50:5.7±2.1µM (Na+/Ca2+exchanger)   体外研究 KB-R7943 mesylate blocks NMDAR-mediated ion currents,and inhibits NMDA-induced increase in cytosolic Ca2+ with IC50=13.4±3.6µM but accelerates calcium deregulation and mitochondrial depolarization in glutamate-treated neurons.KBR7943 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±3.6µM confirming the inhibition of NMDA receptors observed in electrophysiological experiments.wtRyR1-HEK 293 pretreated with KB-R7943 (10μM,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 1mM compared with 0.5 and 0.75mM (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 ~120nM,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.   推荐实验方法(仅供参考) 细胞实验:   EK 293 cells stably expressing the wtRyR1 (wtRyR1-HEK 293) are maintained in Dulbecco's modified Eagle's medium supplemented with 2mM glutamine,100μg/mL streptomycin,100U/mL penicillin,1mM sodium pyruvate,and 10% fetal bovine serum at 37℃ under 5% CO2.wtRyR1-HEK 293 cells are loaded with 5μM Fluo-4 acetoxymethyl ester at 37℃ for 30 min to measure Ca2+ transients in an imaging buffer consisting of 140mM NaCl,5mM KCl,2mM MgCl2,2mM CaCl2,10mM HEPES,and 10mM 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 15s 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.
保存条件：-20℃

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