| 中文名称: | KB-R7943 | ||||
|---|---|---|---|---|---|
| 英文名称: | KB-R7943 | ||||
| 别名: | KB-R7943甲磺酰酸盐 2-[4-[(4-nitrophenyl)methoxy]phenyl]ethyl ester, methanesulfonate (1:1),Carbamimidothioic acid | ||||
| CAS No: | 182004-65-5 | 分子式: | C16H17N3O3S.CH3SO3H | 分子量: | 427.5 |
| CAS No: | 182004-65-5 | ||||
| 分子式: | C16H17N3O3S.CH3SO3H | ||||
| 分子量: | 427.5 | ||||
| MDL: | MFCD00952138 | ||||
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： |
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. |
|
本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)
摩尔浓度计算公式
用本工具协助配置特定浓度的溶液，使用的计算公式为：
开始浓度 x 开始体积 = 最终浓度 x 最终体积
稀释公式
稀释公式一般简略地表示为：C1V1 = C2V2 ( 输入 输出 )
