Flunarizine
Based on 6 publication(s) in Google Scholar
Flunarizine is a potent dual Na+/Ca2+ channel (T-type) blocker. Flunarizine is a D2 dopamine receptor antagonist. Flunarizine shows anticonvulsive and antimigraine activity, and peripheral vasodilator effects.
For research use only. We do not sell to patients.
- Purity: 99.79%
- CAS No.: 52468-60-7
- Formula: C26H26F2N2
- Molecular Weight:404.49
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Flunarizine
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All Calcium Channel Isoforms
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Biological Activity
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D2 Receptor |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | IC50 |
0.49 μM
Compound: Flunarizine
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Inhibitory activity against type IIA sodium channel in CNaIIA-1 cell line expressed in CHO cells
Inhibitory activity against type IIA sodium channel in CNaIIA-1 cell line expressed in CHO cells
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[PMID: 8691482] |
| HEK293 | IC50 |
0.08 μM
Compound: Flunarizine
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Blocking of rat N-type calcium channel alpha-1B/alpha-2-delta-1/beta-1b activity expressed in HEK293 cells assessed as whole cell current by whole cell patch clamp assay
Blocking of rat N-type calcium channel alpha-1B/alpha-2-delta-1/beta-1b activity expressed in HEK293 cells assessed as whole cell current by whole cell patch clamp assay
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[PMID: 19815411] |
| HEK293 | IC50 |
0.31 μM
Compound: Flunarizine
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Blocking of rat Voltage-dependent L-type calcium channel alpha1c/alpha2delta-1/beta1b activity expressed in HEK293 cells assessed as whole cell current by whole cell patch clamp assay
Blocking of rat Voltage-dependent L-type calcium channel alpha1c/alpha2delta-1/beta1b activity expressed in HEK293 cells assessed as whole cell current by whole cell patch clamp assay
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[PMID: 19815411] |
| IMR-32 | IC50 |
0.78 μM
Compound: 3, flunarizine
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Inhibition of calcium channel L type in IMR32 cells
Inhibition of calcium channel L type in IMR32 cells
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[PMID: 17134896] |
| IMR-32 | IC50 |
1.67 μM
Compound: 3, flunarizine
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Inhibition of calcium channel Cav2.2 in IMR32 cells
Inhibition of calcium channel Cav2.2 in IMR32 cells
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[PMID: 17134896] |
Flunarizine blocks sodium currents (INa) and calcium currents (ICa) with IC50 values 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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Chromaffin cells[4]
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Concentration:10 and 30 μM
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Incubation Time:24 hours
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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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male BALB/c mice (6-8 weeks old) with acute lung injury induced by lipopolysaccharide[5]
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Dosage:30 mg/kg
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Administration:Intraperitoneal injection; 30 mg/kg; once
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Result:Suppressed the LPS-induced cell influx, protein leakage, and inflammatory cytokines release.
Inhibited the pulmonary inflammation.
Chemical Information
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CAS No. 52468-60-7
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Appearance Solid
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Molecular Weight 404.49
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Formula C26H26F2N2
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Color White to off-white
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SMILES
FC1=CC=C(C(N2CCN(C/C=C/C3=CC=CC=C3)CC2)C4=CC=C(F)C=C4)C=C1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (6)
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Journal Impact Factor
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Most Recent
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Phytomedicine
Xiongshao Zhitong granules alleviate nitroglycerin-induced migraine by regulating the TRPV1-mediated NLRP3 inflammatory pathway in rats. [Abstract]2025 Apr 11:142:156754. PMID: 40252439 -
J Headache Pain
Ex vivo stimulation of the trigeminal nucleus caudalis induces peripheral CGRP release in the trigeminal ganglion and reveals a distinct dopamine-endocannabinoid mechanism relevant to migraine. [Abstract]2025 Jun 16;26(1):141. PMID: 40524163 -
J Ethnopharmacol
Evodiamine via targeting nNOS and AMPA receptor GluA1 inhibits nitroglycerin-induced migraine-like response. [Abstract]2020 May 23;254:112727. PMID: 32147481 -
Sci Rep
2018 Nov 16;8(1):16932. PMID: 30446677
Flunarizine purchased from MedChemExpress. Usage Cited in: Sci Rep. 2018 Nov 16;8(1):16932. [Abstract]
Western blot analysis of SUM149PT cells treated by FLN (20 μM, 48 h).
Flunarizine purchased from MedChemExpress. Usage Cited in: Sci Rep. 2018 Nov 16;8(1):16932. [Abstract]
FLN enhances autophagic influx and N-Ras translocation to autophagosomes. Cells co-transfected with mCherry-N-Ras and EGFP-LC3 are imaged by confocal microscopy after FLN treatment.
Flunarizine purchased from MedChemExpress. Usage Cited in: Sci Rep. 2018 Nov 16;8(1):16932. [Abstract]
SUM149PT cells are first treated with FLN as in panel-A, followed by autophagy inhibitors 3-MA (5 mM), chloroquine (20 μM) or bafilomycin A1 (20 nM) for another 24 hours. The proteasome inhibitor MG132 (15 μM) is included as a negative control to show unabated N-Ras reduction. The cells are then harvested and analyzed by Western blot.
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J Leukoc Biol
Flunarizine suppresses Mycobacterium tuberculosis growth via calmodulin-dependent phagosome maturation. [Abstract]2022 May;111(5):1021-1029. PMID: 34533236 -
Solvent & Solubility
DMSO : 100 mg/mL (247.22 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.18 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (277 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Hong-Seob So, et al. Protective effect of T-type calcium channel blocker flunarizine on cisplatin-induced death of auditory cells. Hear Res. 2005 Jun;204(1-2):127-39. [Content Brief]
[2]. Qing Ye, et al. Flunarizine blocks voltage-gated Na(+) and Ca(2+) currents in cultured rat cortical neurons: A possible locus of action in the prevention of migraine. Neurosci Lett. 2011 Jan 10;487(3):394-9. [Content Brief]
[3]. Celia M Santi, et al. Differential inhibition of T-type calcium channels by neuroleptics. J Neurosci. 2002 Jan 15;22(2):396-403. [Content Brief]
[4]. Novalbos J, et al. Effects of dotarizine and flunarizine on chromaffin cell viability and cytosolic Ca2+. Eur J Pharmacol. 1999 Feb 5;366(2-3):309-17. [Content Brief]
[5]. Wan L, et al. Mibefradil and Flunarizine, Two T-Type Calcium Channel Inhibitors, Protect Mice against Lipopolysaccharide-Induced Acute Lung Injury. Mediators Inflamm. 2020 Nov 10;2020:3691701. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.4722 mL | 12.3612 mL | 24.7225 mL | 61.8062 mL |
| 5 mM | 0.4944 mL | 2.4722 mL | 4.9445 mL | 12.3612 mL | |
| 10 mM | 0.2472 mL | 1.2361 mL | 2.4722 mL | 6.1806 mL | |
| 15 mM | 0.1648 mL | 0.8241 mL | 1.6482 mL | 4.1204 mL | |
| 20 mM | 0.1236 mL | 0.6181 mL | 1.2361 mL | 3.0903 mL | |
| 25 mM | 0.0989 mL | 0.4944 mL | 0.9889 mL | 2.4722 mL | |
| 30 mM | 0.0824 mL | 0.4120 mL | 0.8241 mL | 2.0602 mL | |
| 40 mM | 0.0618 mL | 0.3090 mL | 0.6181 mL | 1.5452 mL | |
| 50 mM | 0.0494 mL | 0.2472 mL | 0.4944 mL | 1.2361 mL | |
| 60 mM | 0.0412 mL | 0.2060 mL | 0.4120 mL | 1.0301 mL | |
| 80 mM | 0.0309 mL | 0.1545 mL | 0.3090 mL | 0.7726 mL | |
| 100 mM | 0.0247 mL | 0.1236 mL | 0.2472 mL | 0.6181 mL |
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