货号:A165907 同义名: Flunarizine (hydrochloride);KW-3149
Flunarizine 2HCl is a dual Na+/Ca2+ channel (T-type) blocker with neuroprotective property.
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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 | ✔ | 95% | |||||||||||||||||
Zegocractin |
++
Orai1/STIM1-mediated Ca2+ currents, IC50: 120 nM |
99%+ | |||||||||||||||||
Tanshinone IIA sulfonate sodium | ✔ | 98% | |||||||||||||||||
Ulixacaltamide |
++
hCaV3.1, IC50: 50 nM hCaV3.2, IC50: 110 nM |
99%+ | |||||||||||||||||
Dronedarone Hydrochloride | ✔ | 95% | |||||||||||||||||
Nitrendipine |
+
Calcium channel, IC50: 95 nM |
98% | |||||||||||||||||
Efonidipine HCl monoethanolate | ✔ | 98% | |||||||||||||||||
Cinnarizine | ✔ | 98% | |||||||||||||||||
SEA0400 |
++
NCX, IC50: 33 nM |
ERK,p38 MAPK,ROS | 99%+ | ||||||||||||||||
Fasudil HCl | ✔ | Rho,PKA | 98% | ||||||||||||||||
ML-9 | ✔ | MLCK,Akt | 99%+ | ||||||||||||||||
Flunarizine 2HCl |
+
Calcium channel, Ki: 68 nM |
95% | |||||||||||||||||
Lomerizine 2HCl | ✔ | 98% | |||||||||||||||||
Efonidipine | ✔ | 98% | |||||||||||||||||
Levamlodipine | ✔ | 97% | |||||||||||||||||
Nisoldipine |
++
L-type Cav1.2, IC50: 10 nM |
97% | |||||||||||||||||
Isradipine | ✔ | 98% | |||||||||||||||||
Lacidipine | ✔ | 98% | |||||||||||||||||
Lercanidipine | ✔ | 98% | |||||||||||||||||
Loureirin B | ✔ | Potassium Channel | 99%+ | ||||||||||||||||
Tetracaine HCl | ✔ | 98% | |||||||||||||||||
Manidipine |
+++
Calcium channel, IC50: 2.6 nM |
98% | |||||||||||||||||
Manidipine Dihydrochlorid |
+++
Calcium channel, IC50: 2.6 nM |
98% | |||||||||||||||||
Nicardipine | ✔ | 98% | |||||||||||||||||
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 | ✔ | 98% | |||||||||||||||||
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 | ✔ | 98% | |||||||||||||||||
Cinepazide Maleate | ✔ | 98% | |||||||||||||||||
Terfenadine | ✔ | 98% | |||||||||||||||||
YM-58483 | ✔ | 99%+ | |||||||||||||||||
Ranolazine | ✔ | 98% | |||||||||||||||||
Praeruptorin A | ✔ | p38 MAPK,Akt | 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。 |
靶点 |
|
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]. |
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 << |
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 |
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 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Inert atmosphere,2-8°C |
溶解度 |
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 |
动物实验配方 |