Flunarizine dihydrochloride 是一种有效的Na+/Ca2+(T 型) 通道双重阻滞剂。Flunarizine dihydrochloride 是D2多巴胺受体拮抗剂。Flunarizine dihydrochloride 具有抗惊厥和抗偏头痛活性,以及外周血管扩张作用。
生物活性 | Flunarizine dihydrochloride is a potent dualNa+/Ca2+channel (T-type)blocker. Flunarizine dihydrochloride is aD2dopaminereceptor antagonist. Flunarizine dihydrochloride shows anticonvulsive and antimigraine activity, and peripheral vasodilator effects[1][2][3][4][5]. |
IC50& Target[1][3] | T-type calcium channel | D2Receptor |
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体外研究 (In Vitro) | Flunarizine blocks sodium currents (INa) and calcium currents (ICa) with IC50values of 0.94 μM and 1.77 μM in cultured rat cortical neurons, respectively[2]. Flunarizine (10 and 30 μM; 24 h) shows cytotoxic effects to chromaffin cells[4]. Flunarizine (1-30 μM) causes clear cytoprotection of chromaffin cell at concentrations of 3-10 μM[4].
Cell Viability Assay[4] Cell Line: | Chromaffin cells | Concentration: | 10 and 30 μM | Incubation Time: | 24 hours | Result: | Showed a tendency to increase cell death at the concentration of 10 μM, and showed near 100% cell loss at the concentration of 30 μM. |
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体内研究 (In Vivo) | Flunarizine (intraperitoneal injection; 30 mg/kg; once) protects mice from lipopolysaccharide- (LPS-) induced acute lung injury (ALI)[5].
Animal Model: | Male BALB/c mice (6-8 weeks old) with acute lung injury induced by lipopolysaccharide[5] | Dosage: | 30 mg/kg | Administration: | Intraperitoneal injection; 30 mg/kg; once | Result: | Suppressed the LPS-induced cell influx, protein leakage, and inflammatory cytokines release. Inhibited the pulmonary inflammation. |
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运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
溶解性数据 | In Vitro: DMSO : 50 mg/mL(104.73 mM;Need ultrasonic) H2O : 1 mg/mL(2.09 mM;Need ultrasonic) 配制储备液 1 mM | 2.0946 mL | 10.4730 mL | 20.9459 mL | 5 mM | 0.4189 mL | 2.0946 mL | 4.1892 mL | 10 mM | 0.2095 mL | 1.0473 mL | 2.0946 mL |
*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。 储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro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. 请依序添加每种溶剂: PBS Solubility: 10 mg/mL (20.95 mM); Clear solution; Need ultrasonic 2. 请依序添加每种溶剂: 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.5 mg/mL (5.24 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (5.24 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。 3. 请依序添加每种溶剂: 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.5 mg/mL (5.24 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (5.24 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 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。 4. 请依序添加每种溶剂: 10% DMSO 90%corn oil Solubility: ≥ 2.5 mg/mL (5.24 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (5.24 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。 *以上所有助溶剂都可在本网站选购。
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