| Size | Price | Stock | Qty |
|---|---|---|---|
| 500mg |
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| Other Sizes |
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| ln Vitro |
In cultured cortical neurons, flunarizine dihydrochloride has an IC50 value of 1.77 μM for calcium current (ICa) and 0.94 μM for sodium current (INa) expansion [2]. At concentrations of 3–10 μM, flunarizine dihydrochloride (10 and 30 μM; 24 Flunarizine hydrochloride (1–30 μM) significantly damages chromaffin cells [4]. Chromaffin cells are significantly cytotoxically affected by cell viability, which is assessed in [4] hours [4].
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|---|---|
| ln Vivo |
Flunarizine dihydrochloride (intraperitoneal injection; 30 mg/kg; once) protects against lipopolysaccharide (LPS)-induced acute lung injury (ALI) in the neck of mice [5].
|
| Cell Assay |
Cell Viability Assay[4]
Cell Types: Chromaffin Tested Concentrations: 10 and 30 μM Incubation Duration: 24 hrs (hours) Experimental Results: demonstrated a trend of increased cell death at 10 μM concentration and close to 100% cell loss at 30 μM concentration. |
| Animal Protocol |
Animal/Disease Models: Male balb/c (Bagg ALBino) mouse (6-8 weeks old)) lipopolysaccharide-induced acute lung injury [5]
Doses: 30 mg/kg Route of Administration: intraperitoneal (ip) injection; 30 mg/kg; Experimental Results:Inhibition of LPS induction of cell influx, protein leakage, and inflammatory cytokine release. Suppress lung inflammation. |
| 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.
[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. [3]. Celia M Santi, et al. Differential inhibition of T-type calcium channels by neuroleptics. J Neurosci. 2002 Jan 15;22(2):396-403. [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. [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. |
| Molecular Formula |
C26H26F2N2.2(HCL)
|
|---|---|
| Molecular Weight |
477.42
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| CAS # |
30484-77-6
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| Related CAS # |
Flunarizine;52468-60-7
|
| SMILES |
FC1=CC=C(C(N2CCN(C/C=C/C3=CC=CC=C3)CC2)C4=CC=C(F)C=C4)C=C1.Cl.Cl
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO : ~50 mg/mL (~104.73 mM)
H2O : ~1 mg/mL (~2.09 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.24 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.24 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (5.24 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 10 mg/mL (20.95 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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