Flunarizine dihydrochloride
Based on 6 publication(s) in Google Scholar
Flunarizine dihydrochloride is a potent dual Na+/Ca2+ channel (T-type) blocker. Flunarizine dihydrochloride is a D2 dopamine receptor antagonist. Flunarizine dihydrochloride shows anticonvulsive and antimigraine activity, and peripheral vasodilator effects.
For research use only. We do not sell to patients.
- Purity: 99.90%
- CAS No.: 30484-77-6
- Formula: C26H28Cl2F2N2
- Molecular Weight:477.42
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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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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Publications Citing Use of MedChemExpress (MCE) Flunarizine dihydrochloride
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All Calcium Channel Isoforms
MoreAll Dopamine Receptor Isoforms
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Biological Activity
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T-type calcium channel |
D2 Receptor |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Caco-2 | CC50 |
136.76 μM
Compound: FLUNARIZINE
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Toxicity against Caco-2 cells determined at 48 hours by intracellular ATP concentration using the CellTiter-Glo Luminescent Cell Viability Assay
Toxicity against Caco-2 cells determined at 48 hours by intracellular ATP concentration using the CellTiter-Glo Luminescent Cell Viability Assay
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10.21203/rs.3.rs-23951/v1 |
| Caco-2 | IC50 |
19.05 μM
Compound: FLUNARIZINE
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Determination of IC50 values for inhibition of SARS-CoV-2 induced cytotoxicity of Caco-2 cells after 48 hours by high content imaging
Determination of IC50 values for inhibition of SARS-CoV-2 induced cytotoxicity of Caco-2 cells after 48 hours by high content imaging
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10.21203/rs.3.rs-23951/v1 |
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].
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Flunarizine (10 and 30 μM; 24 h) shows cytotoxic effects to chromaffin cells[4].
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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
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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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 30484-77-6
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Appearance Solid
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Molecular Weight 477.42
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Formula C26H28Cl2F2N2
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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.Cl.Cl
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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 Jul: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 dihydrochloride 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 dihydrochloride 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 dihydrochloride 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 : 50 mg/mL (104.73 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 1 mg/mL (2.09 mM; Need ultrasonic)
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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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 (5.24 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.24 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 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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: PBS
Solubility: 10 mg/mL (20.95 mM); Clear solution; Need ultrasonic
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. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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 (278 KB)
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SDS (392 KB)
- English - EN (392 KB)
- Français - FR (392 KB)
- Deutsch - DE (392 KB)
- Norwegian - NO (392 KB)
- Español - ES (392 KB)
- Swedish - SV (392 KB)
- Italian - IT (392 KB)
- Korean - KR (392 KB)
- Portuguese - PT (392 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 (sealed storage, away from moisture). 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 |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 2.0946 mL | 10.4730 mL | 20.9459 mL | 52.3648 mL |
| DMSO | 5 mM | 0.4189 mL | 2.0946 mL | 4.1892 mL | 10.4730 mL |
| 10 mM | 0.2095 mL | 1.0473 mL | 2.0946 mL | 5.2365 mL | |
| 15 mM | 0.1396 mL | 0.6982 mL | 1.3964 mL | 3.4910 mL | |
| 20 mM | 0.1047 mL | 0.5236 mL | 1.0473 mL | 2.6182 mL | |
| 25 mM | 0.0838 mL | 0.4189 mL | 0.8378 mL | 2.0946 mL | |
| 30 mM | 0.0698 mL | 0.3491 mL | 0.6982 mL | 1.7455 mL | |
| 40 mM | 0.0524 mL | 0.2618 mL | 0.5236 mL | 1.3091 mL | |
| 50 mM | 0.0419 mL | 0.2095 mL | 0.4189 mL | 1.0473 mL | |
| 60 mM | 0.0349 mL | 0.1745 mL | 0.3491 mL | 0.8727 mL | |
| 80 mM | 0.0262 mL | 0.1309 mL | 0.2618 mL | 0.6546 mL | |
| 100 mM | 0.0209 mL | 0.1047 mL | 0.2095 mL | 0.5236 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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