| Size | Price | Stock | Qty |
|---|---|---|---|
| 100mg |
|
||
| 250mg |
|
||
| 500mg |
|
||
| 1g |
|
||
| 2g |
|
||
| 5g |
|
||
| Other Sizes |
|
Purity: ≥98%
Flunarizine 2HCl (formerly R-14950; KW3149; R14950; KW 3149; trade name Sibelium), the dihydrochloride salt form of Flunarizine, is a selective calcium entry/channel blocker with calmodulin binding properties and anti-histamine H1 activity. It blocks alcium channel with a Ki of 68 nM. Flunarizine is authorized for use as an adjuvant in the treatment of epilepsy, as well as in the prophylaxis of migraine, occlusive peripheral vascular disease, and vertigo of both central and peripheral origin.
| Targets |
T-type calcium channel; D2 Receptor
|
|---|---|
| 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].
|
| ln Vivo |
Acute lung damage (ALI) caused by lipopolysaccharide (LPS) in mice's necks is prevented by flunarizine dihydrochloride (intraperitoneal injection; 30 mg/kg; once) [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 |
C26H26F2N2.2HCL
|
|
|---|---|---|
| Molecular Weight |
477.42
|
|
| Exact Mass |
476.16
|
|
| Elemental Analysis |
C, 65.41; H, 5.91; Cl, 14.85; F, 7.96; N, 5.87
|
|
| CAS # |
22348-32-9
|
|
| Related CAS # |
|
|
| Appearance |
Solid powder
|
|
| SMILES |
C1C[C@@H](NC1)C(C2=CC=CC=C2)(C3=CC=CC=C3)O
|
|
| InChi Key |
OGCGXUGBDJGFFY-MRXNPFEDSA-N
|
|
| InChi Code |
InChI=1S/C17H19NO/c19-17(16-12-7-13-18-16,14-8-3-1-4-9-14)15-10-5-2-6-11-15/h1-6,8-11,16,18-19H,7,12-13H2/t16-/m1/s1
|
|
| Chemical Name |
diphenyl-[(2R)-pyrrolidin-2-yl]methano
|
|
| Synonyms |
|
|
| HS Tariff Code |
2934.99.9001
|
|
| 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) |
|
|||
|---|---|---|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| 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.
|
|
|
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
COA
