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KB-R7943 mesylate
目录号: PC11872 纯度: ≥98%
CAS No. :182004-65-5
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中文名称
KB-R7943 mesylate
中文别名
S-[4-[(4-硝基苄基)氧代]苯乙基]异硫脲甲磺酸盐;2-[2-[4-(4-硝基苄氧基)苯基]乙基]异硫脲甲烷磺;3,3,4,4-四氟吡咯烷盐酸盐;KB-R7943 甲磺酰酸盐;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;KB-R7943 甲磺酸盐;4-[(4-硝基苄基)氧代]苯乙基甲胺酰亚胺硫醇甲磺酸盐
英文名称
KB-R7943 mesylate
英文别名
2-[2-[4-(4-NITROBENZYLOXY)PHENYL]ETHYL]ISOTHIOUREA MESYLATE;S-[4-[(4-Nitrobenzyl)oxy]phenethyl]isothiourea Methanesulfonate;4-((4-Nitrobenzyl)oxy)phenethyl carbamimidothioate methanesulfonate;KB-R7943;KB-R7943 (mesylate);KB-R7943 MESYLATE;KB-R7943 MESYLATE KB-R7943;KB-R7943 MESYLATE KB-R7943;methanesulfonic acid,2-[4-[(4-nitrophenyl)methoxy]phenyl]ethyl carbamimidothioate;4-[(4-Nitrobenzyl)oxy]phenethyl Carbamimidothioate Methanesulfonate;Carbamimidothioic Acid 4-[(4-Nitrobenzyl)oxy]phenethyl Ester Methanesulfonate;HMS3267H09;Carbamimidothioic acid 2-[4-[(4-nitrophenyl)methoxy]phenyl]ethyl ester methanesulfonate;Carbamimidothioic acid 2-[4-[(4-nitrophenyl)methoxy]phenyl]ethyl ester monomethanesulfonate;2-(2-(4-(4-NITROBENZYLOXY)PHENYL)ETHYL)ISOTHIOUREA, METHANE SULFONATE;KB-R 7943;4-((4-Nitrobenzyl)oxy)phenethyl carbamimidothioatemethanesulfonate;GTPL4232;CT
Cas No.
182004-65-5
分子式
C17H21N3O6S2
分子量
427.50
包装储存

Sealed and stored at 4℃,, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

生物活性

KB-R7943 mesylate is a widely used inhibitor of the reverse Na/Ca exchanger (NCXrev) with IC50 of 5.7±2.1 μM. KB-R7943 mesylate induces cancer cell death via activating the JNK pathway and blocking autophagic flux.

性状

Solid

IC50 & Target[1][2]

IC50: 5.7±2.1 μM (Na/Ca exchanger)

体外研究(In Vitro)

KB-R7943 mesylate blocks NMDAR-mediated ion currents, and inhibits NMDA-induced increase in cytosolic Ca with IC50=13.4±3.6 μM but accelerates calcium deregulation and mitochondrial depolarization in glutamate-treated neurons. KB-R7943 depolarizes mitochondria in a Ca-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 [Ca]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 Ca 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.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature or refrigerated transportation.

储存方式

Sealed and stored at 4℃,, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

参考文献
溶解度数据
体外研究: 

DMSO : 100 mg/mL (233.92 mM; Need ultrasonic)

配制储备溶液
浓度 溶剂体积 质量 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
*

产品不同,其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液;配成溶液后,建议分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时,建议在 6 个月内使用,-20°C 储存时,建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    建议依照次序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (5.85 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.85 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH?O 中,得到澄清透明的生理盐水溶液
  • 2.

    建议依照次序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (5.85 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.85 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 3.

    建议依照次序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.85 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.85 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*
搜索质检报告(COA)

1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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