中文名 | KB-R7943甲磺酰酸盐 |
英文名 | 2-[2-[4-(4-NITROBENZYLOXY)PHENYL]ETHYL]ISOTHIOUREA MESYLATE |
别名 | 化合物KB-R7943 KB-R7943 甲磺酸盐 KB-R7943甲磺酰酸盐 KB-R7943 甲磺酰酸盐 4-[(4-硝基苄基)氧代]苯基乙基]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 |
英文别名 | KB-R7943 KB-R7943 MESYLATE 2-[2-[4-(4-NITROBENZYLOXY)PHENYL]ETHYL]ISOTHIOUREA MESYLATE S-[4-[(4-Nitrobenzyl)oxy]phenethyl]isothiourea Methanesulfonate 4-((4-Nitrobenzyl)oxy)phenethyl carbaMiMidothioate Methanesulfonate 2-(2-(4-(4-NITROBENZYLOXY)PHENYL)ETHYL)ISOTHIOUREA, METHANE SULFONATE Carbamimidothioic acid 2-[4-[(4-nitrophenyl)methoxy]phenyl]ethyl ester methanesulfonate Carbamimidothioic acid 2-[4-[(4-nitrophenyl)methoxy]phenyl]ethyl ester monomethanesulfonate |
CAS | 182004-65-5 |
化学式 | C17H21N3O6S2 |
分子量 | 427.5 |
InChI | InChI=1/C16H17N3O3S.CH4O3S/c17-16(18)23-10-9-12-3-7-15(8-4-12)22-11-13-1-5-14(6-2-13)19(20)21;1-5(2,3)4/h1-8H,9-11H2,(H3,17,18);1H3,(H,2,3,4) |
熔点 | >214°C (dec.) |
沸点 | 534.6°C at 760 mmHg |
闪点 | 277.1°C |
蒸汽压 | 1.67E-11mmHg at 25°C |
溶解度 | 溶于DMSO (高达50 mg/ml)。 |
存储条件 | Inert atmosphere,2-8°C |
稳定性 | 从提供的购买之日起稳定2年。DMSO中的溶液可以在-20 °C下储存长达3个月。 |
外观 | 白色结晶固体 |
颜色 | Tan |
体外研究 | 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. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.339 ml | 11.696 ml | 23.392 ml |
5 mM | 0.468 ml | 2.339 ml | 4.678 ml |
10 mM | 0.234 ml | 1.17 ml | 2.339 ml |
5 mM | 0.047 ml | 0.234 ml | 0.468 ml |
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