KB-R7943 甲磺酰酸盐
中文名称 | KB-R7943 甲磺酰酸盐 |
---|---|
中文同义词 | KB-R7943 甲磺酰酸盐;KB-R7943 甲磺酸盐;S-[4-[(4-硝基苄基)氧代]苯乙基]异硫脲甲磺酸盐;S-[4-[(4-硝基苄基)氧代]苯乙基]异硫脲甲磺酸盐;S-[4-[(4-NITROBENZYL)OXY]PHENETHYL]ISOTHIOUREA METHANESULFONATE S-[4-[(4-硝基苄基)氧代]苯乙基]异硫脲甲磺酸盐;S-[4-[(4-硝基苄基)氧代]苯乙基]异硫脲甲磺酸盐(易制爆,甄准不供应);化合物KB-R7943;4-[(4-硝基苄基)氧代]苯基乙基]异硫脲甲磺酸盐 |
英文名称 | 2-[2-[4-(4-NITROBENZYLOXY)PHENYL]ETHYL]ISOTHIOUREA MESYLATE |
英文同义词 | Carbamimidothioic acid 2-[4-[(4-nitrophenyl)methoxy]phenyl]ethyl ester methanesulfonate;Carbamimidothioic acid 2-[4-[(4-nitrophenyl)methoxy]phenyl]ethyl ester monomethanesulfonate;KB-R7943;KB-R7943 MESYLATE;2-[2-[4-(4-NITROBENZYLOXY)PHENYL]ETHYL]ISOTHIOUREA MESYLATE;2-(2-(4-(4-NITROBENZYLOXY)PHENYL)ETHYL)ISOTHIOUREA, METHANE SULFONATE;S-[4-[(4-Nitrobenzyl)oxy]phenethyl]isothiourea Methanesulfonate;4-((4-Nitrobenzyl)oxy)phenethyl carbaMiMidothioate Methanesulfonate |
CAS号 | 182004-65-5 |
分子式 | C17H21N3O6S2 |
分子量 | 427.49 |
EINECS号 | |
相关类别 | 定制化学品;叠氮;偶氮;重氮化合物;Signalling;Ion transporter and other ion channel |
Mol文件 | 182004-65-5.mol |
结构式 |
KB-R7943 甲磺酰酸盐 性质
熔点 | >214°C (dec.) |
---|---|
储存条件 | Inert atmosphere,2-8°C |
溶解度 | 溶于DMSO(高达50mg/ml)。 |
形态 | 白色结晶固体 |
颜色 | 棕褐色 |
稳定性 | 可在-20°C下的DMSO中的溶液储存长达3个月。 |
IC50: 5.7±2.1 µM (Na + /Ca 2+ exchanger)
KB-R7943 mesylate blocks NMDAR-mediated ion currents, and inhibits NMDA-induced increase in cytosolic Ca 2+ with IC 50 =13.4±3.6 µM but accelerates calcium deregulation and mitochondrial depolarization in glutamate-treated neurons. KB-R7943 depolarizes mitochondria in a Ca 2+ -independent manner. KB-R7943 inhibits 2,4-dinitrophenol-stimulated respiration of cultured neurons with IC 50 =11.4±2.4 µM. In addition to NCX rev , KB-R7943 dose-dependently and reversibly blocked ion currents elicited by NMDA. KB-R7943 dose-dependently inhibits NMDA-induced increases in [Ca 2+ ] c with IC 50 =13.4±3.6 µM confirming the inhibition of NMDA receptors observed in electrophysiological experiments. wt RyR1-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 Ca 2+ 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 I hERG and native I Kr rapidly on membrane depolarization with IC 50 values of ~89 and ~120 nM, respectively, for current tails at −40 mV following depolarizing voltage commands to +20 mV. I hERG inhibition by KB-R7943 exhibits both time- and voltage-dependence but shows no preference for inactivated over activated channels.
安全信息
海关编码 | 2930.90.2900 |
---|
更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
---|---|---|---|---|---|
2024/08/19 | HY-15415 | KB-R7943 mesylate | 5 mg | 493元 | |
2024/08/19 | HY-15415 | KB-R7943 甲磺酰酸盐 KB-R7943 mesylate | 182004-65-5 | 10mg | 790元 |