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/ Calcium Channel / Flunarizine 2HCl

盐酸氟桂利嗪 /Flunarizine 2HCl {[allProObj[0].p_purity_real_show]}

货号：A165907 同义名： Flunarizine (hydrochloride);KW-3149

Flunarizine 2HCl is a dual Na+/Ca2+ channel (T-type) blocker with neuroprotective property.

Flunarizine 2HCl 化学结构 CAS号：30484-77-6
Flunarizine 2HCl 化学结构
CAS号：30484-77-6
Flunarizine 2HCl 3D分子结构
CAS号：30484-77-6
Flunarizine 2HCl 化学结构 CAS号：30484-77-6
Flunarizine 2HCl 3D分子结构 CAS号：30484-77-6
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Flunarizine 2HCl 纯度/质量文件 产品仅供科研

货号：A165907 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

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产品名称 Ca2+ channel-like protein ↓ Calcium Channel ↓ Cav 2.2 ↓ 其他靶点 纯度
CDC25B-IN-2 ✔ Akt 99%+
Clevidipine ✔ 97%
Verapamil HCl ✔ 99%
Amlodipine ✔ 99%
Amlodipine maleate ✔ 98%
(+)-cis-Diltiazem HCl ✔ 99%
Zegocractin ++

Orai1/STIM1-mediated Ca2+ currents, IC50: 120 nM

 		99%+
Tanshinone IIA sulfonate sodium ✔ 98%
Ulixacaltamide ++

hCaV3.2, IC50: 110 nM

hCaV3.1, IC50: 50 nM

 		99%+
Dronedarone Hydrochloride ✔ 95%
Nitrendipine +

Calcium channel, IC50: 95 nM

 		98%
Efonidipine HCl monoethanolate ✔ 98%
Cinnarizine ✔ 98%
SEA0400 ++

NCX, IC50: 33 nM

 		p38 MAPK,ERK,ROS 99%+
Fasudil HCl ✔ PKA,Rho 98%
ML-9 ✔ Akt,MLCK 99%+
Flunarizine 2HCl +

Calcium channel, Ki: 68 nM

 		95%
Lomerizine 2HCl ✔ 98%
Efonidipine ✔ 98%
Levamlodipine ✔ 98%
Nisoldipine ++

L-type Cav1.2, IC50: 10 nM

 		97%
Isradipine ✔ 98%
Lacidipine ✔ 98%
Lercanidipine ✔ 99%
Loureirin B ✔ Potassium Channel 99%+
Tetracaine HCl ✔ 98%
Manidipine +++

Calcium channel, IC50: 2.6 nM

 		99%
Manidipine Dihydrochlorid +++

Calcium channel, IC50: 2.6 nM

 		98%
Nicardipine ✔ 99%
Wilforgine ✔ 98+%
Econazole ✔ 99%+
Ginsenoside Rd ✔ NF-κB 98%
Fendiline HCl ✔ 98+%
Mesaconitine ✔ 98%
Tetrandrine ✔ 95%
Nifedipine ✔ 95%
Nilvadipine ++++

Calcium channel, IC50: 0.03 nM

 		98%
Barnidipine ++++

[3H]nitrendipine, Ki: 0.21 nM

 		95+%
Azelnidipine ✔ 97%
Levetiracetam ✔ 98%
Nimodipine ✔ 95%
Benidipine HCl ✔ 98%
Pinaverium bromide ✔ 98%
Pranidipine ✔ 99%
NP118809 +

L-type calcium channel, IC50: 12.2 μM

N-type Ca2+ channel, IC50: 0.11 μM

 		98%
Amlodipine Besylate +++

Calcium channel, IC50: 1.9 nM

 		97%
Cilnidipine ✔ 99%
Cinepazide Maleate ✔ 99% (HPLC)
Terfenadine ✔ 98%
YM-58483 ✔ 99%+
Ranolazine ✔ 98%
Praeruptorin A ✔ Akt,p38 MAPK 98%
Ranolazine 2HCl ✔ 98%
Felodipine ++++

L-type calcium channel, IC50: 0.15 nM

 		98%
PD173212 +++

N-type Ca2+ channel, IC50: 36 nM

 		98%
Levamlodipine besylate ✔ 97%
Carboxyamidotriazole Orotate ✔ 98%
IGS-1.76 ✔ 98+%
WH-4-023 ++++

Cav 2.2, IC50: 0.001 μM

 		++++

Cav 2.2, IC50: 0.001 μM

 		99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Flunarizine 2HCl 生物活性

靶点

  • Calcium Channel

    Calcium channel, Ki:68 nM
描述 Flunarizine dihydrochloride (FHC), a calcium antagonist, is used for the prophylaxis to migraine. The solubility of the poorly soluble FHC was successfully improved by preparing it as a nano emulsion[3]. The most common indication for flunarizine use was chronic migraine, followed by migraine with aura, sporadic hemiplegic migraine, familial hemiplegic migraine and new daily persistent headache with migrainous features. The most common dose used was 10 mg per day. The most common adverse events were tiredness, mood change and weight gain[4]. Moreover, benefit of flunarizine prophylaxis on headache severity, frequency, and duration in children with Sturge-Weber syndrome without severe side effects[5]. In an 8-week study, 10 mg/d flunarizine is more effective than 50 mg/d topiramate for CM (Chronic migraine) prophylaxis in patients[6]. Adding tSNS (transcutaneous supraorbital neurostimulation) to flunarizine can improve the therapeutic efficacy of migraine prophylaxis without increasing the adverse effects[7].

Flunarizine 2HCl 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT03461874 Migraine Without Aura Not Applicable Recruiting July 15, 2021 Italy ... 展开 >> Fondazione IRCCS Istituto Neurologico C. Besta, Neuroalgology Unit Recruiting Milano, Italy, 20133 Contact: Licia Grazzi, MD       licia.grazzi@istituto-besta.it    Principal Investigator: Licia Grazzi, MD 收起 <<
NCT02580968 Migraine Not Applicable Completed - China ... 展开 >> Longhua Hospital,Shanghai University of Traditional Chinese Medicine Shanghai, China, 200032 收起 <<
NCT02747940 Chronic Pain ... 展开 >>Chronic Migraine Fibromyalgia 收起 << Phase 4 Recruiting - Taiwan ... 展开 >> Headache Center, Teipei Veterans General Hospital Recruiting Taipei, Taiwan, 112 Contact: Shuu-Jiun Wang, MD    +886-2-28712121 ext 2425    sjwang@vghtpe.gov.tw    Contact: Jong-Ling Fuh, MD    +886-2-28712121 ext 3256    jlfuh@vghtpe.gov.tw    Principal Investigator: Shuu-Jiun Wang, MD 收起 <<

Flunarizine 2HCl 参考文献

[1]Kotake H, Kinugawa T, et al.Actions of flunarizine dihydrochloride on the electrical activity of isolated guinea-pig papillary muscle and rabbit sino-atrial node. Res Commun Chem Pathol Pharmacol. 1988 Nov;62(2):147-60.

[2]Fagbemi O, Kane KA, et al. The effects of verapamil, prenylamine, flunarizine and cinnarizine on coronary artery occlusion-induced arrhythmias in anaesthetized rats. Br J Pharmacol. 1984 Sep;83(1):299-304.

[3]Newton MJ, Harjot K. Fabrication, Characterization, In vitro Evaluation of Solid Lipid Nanoemulsion of Flunarizine dihydrochloride for Nasal Delivery. Antiinflamm Antiallergy Agents Med Chem. 2017; 15(3):204‐220

[4]Karsan N, Palethorpe D, Rattanawong W, Marin JC, Bhola R, Goadsby PJ. Flunarizine in migraine-related headache prevention: results from 200 patients treated in the UK. Eur J Neurol. 2018; 25(6):811‐817

[5]Gallop F, Fosi T, Prabhakar P, Aylett SE. Flunarizine for Headache Prophylaxis in Children With Sturge-Weber Syndrome. Pediatr Neurol. 2019; 93:27‐33

[6]Lai KL, Niddam DM, Fuh JL, et al. Flunarizine versus topiramate for chronic migraine prophylaxis: a randomized trial. Acta Neurol Scand. 2017;135(4):476‐483

[7]Jiang L, Yuan DL, Li M, et al. Combination of flunarizine and transcutaneous supraorbital neurostimulation improves migraine prophylaxis. Acta Neurol Scand. 2019;139(3):276‐283

Flunarizine 2HCl 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.09mL

0.42mL

0.21mL

10.47mL

2.09mL

1.05mL

20.95mL

4.19mL

2.09mL

Flunarizine 2HCl 技术信息

CAS号30484-77-6
分子式C26H28Cl2F2N2
分子量 477.417
别名 Flunarizine (hydrochloride);KW-3149;EINECS 250-216-6;Flunarizine HCl;Flunarizine hydrochloride;R14950;Flunarizine dihydrochloride
运输蓝冰
存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Inert atmosphere,2-8°C
溶解方案

DMSO: 50 mg/mL(104.73 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 1 mg/mL(2.09 mM)，配合低频超声助溶

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的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
方案一
方案二
配制的工作液建议现用现配，短期内尽快用完。 以下溶剂前显示的百分比是指该溶剂在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。
方案一
动物实验配方

Tags: Flunarizine | 30484-77-6 | Membrane Transporter/Ion Channel | Neuronal Signaling | GPCR/G Protein | Calcium Channel | Sodium Channel | Dopamine Receptor | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Flunarizine 2HCl 纯度/质量文件 | Flunarizine 2HCl 亚型比较 | Flunarizine 2HCl 生物活性 | Flunarizine 2HCl 临床数据 | Flunarizine 2HCl 参考文献 | Flunarizine 2HCl 实验方案 | Flunarizine 2HCl 技术信息

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