Art. -Nr.: HY-B1090

Cinnarizine

Name: Cinnarizine
Brand: MedChemExpress
SKU: HY-B1090
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Cinnarizine is an orally active, effective and selective inhibitor of L-type calcium channel Cav1.3 with an IC₅₀ of 1.5 μM (in vestibular hair cells). Cinnarizine can cross the blood-brain barrier and regulate calcium homeostasis and dopamine neurotransmission. Cinnarizine inhibits the influx of calcium ions into smooth muscle cells by blocking L-type calcium channels, thereby relaxing vascular smooth muscle, improving cerebral circulation and reducing blood viscosity, while antagonizing dopamine receptors. Cinnarizine can be used in the study of vestibular vertigo, Meniere's disease and cerebrovascular diseases.

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Reinheit : 99.56%
CAS. Nr.: 298-57-7
Formel: C₂₆H₂₈N₂
Molecular Weight:368.51

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Cinnarizine Chemical Structure

CAS. Nr.: 298-57-7

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Biologische Aktivität
- Beschreibung
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

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Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	9.8 μM Compound: 28	Antiproliferative activity against human A549 cells after 120 hrs by MTT assay Antiproliferative activity against human A549 cells after 120 hrs by MTT assay	[PMID: 16680159]
LoVo	IC₅₀	10.5 μM Compound: 28	Antiproliferative activity against human LoVo cells after 120 hrs by MTT assay Antiproliferative activity against human LoVo cells after 120 hrs by MTT assay	[PMID: 16680159]
MIA PaCa-2	IC₅₀	11.1 μM Compound: 28	Antiproliferative activity against human MIAPaCa2cells after 120 hrs by MTT assay Antiproliferative activity against human MIAPaCa2cells after 120 hrs by MTT assay	[PMID: 16680159]
PC-3	IC₅₀	16.1 μM Compound: 28	Antiproliferative activity against human PC3 cells after 120 hrs by MTT assay Antiproliferative activity against human PC3 cells after 120 hrs by MTT assay	[PMID: 16680159]
U-87MG ATCC	IC₅₀	13.5 μM Compound: 28	Antiproliferative activity against human U87MG cells after 120 hrs by MTT assay Antiproliferative activity against human U87MG cells after 120 hrs by MTT assay	[PMID: 16680159]

In Vitro

Cinnarizine (1.5 μM; transient treatment) inhibits L-type calcium current (I_Ca) in a concentration-dependent manner in the voltage-gated calcium current assay of guinea pig vestibular type II hair cells, and the reversibility decreases with increasing concentration^[1].
Cinnarizine (0.5 μM, 1 μM; transient treatment) significantly inhibits pressure-induced potassium current in the pressure-sensitive potassium current assay of guinea pig vestibular type II hair cells, and the inhibitory effect can be completely blocked by Charybdotoxin (HY-P0191)^[2].
Cinnarizine (1-30 μM; 24 h) stimulates HAC15 cells with angiotensin II, reduces aldosterone concentration and CYP11B2 expression^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay^[3]

Cell Line:

HAC15 cells
Concentration:

1, 3, 10, and 30 μM
Incubation Time:

24 h
Result:

Resulted dose-related reduction in CYP11B2 expression.

In Vivo

Cinnarizine (10 mg/kg; oral; once daily; 6 weeks) induces local hair loss and oral dyskinesia in the parkin knockout model (PK-KO) of female mice, significantly reduced the motor activity of mice, and enhanced striatal dopamine metabolism and compensatory activation of the glutathione system^[4].
Cinnarizine (2-10 mg/kg; intravenous injection; once daily; 30 days) has a dose-dependent pharmacokinetic profile in beagle dogs, causing reversible renal injury at 10 mg/kg, with a significant cumulative effect^[5].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Female C57BL6/129SV parkin knock-out (PK-KO) mice and wild-type (WT) littermates (20-25 g, 14 months old) behavioral and neurochemical model^[4]
Dosage:

10 mg/kg dissolved in drinking water
Administration:

Oral administration via drinking water, once daily for 6 weeks.
Result:

Behavioral Changes: Developed PK-KO mice focal alopecia and bucolingual dyskinesia, with motor activity reduced by 30-40% compared to baseline, while WT mice showed no significant behavioral alterations.
Neurochemical Alterations: Increased striatal dopamine (DA) levels by 26% in PK-KO mice, with DA metabolites DOPAC and HVA elevated by 49% and 19%, respectively. Increased glutathione (GSH/GSSG ratio) by 25% in the striatum, indicating compensatory anti-oxidative stress response.
Protein Expression: Decreased tyrosine hydroxylase (TH) protein levels by 15% in PK-KO striatum, while β-tubulin increased by 20%. Pro-apoptotic proteins Bax and Bclx ratio indicated enhanced neuronal apoptosis in PK-KO mice treated with cinnarizine.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 298-57-7
Appearance Solid
Molecular Weight 368.51
Formel C₂₆H₂₈N₂
Color White to off-white
SMILES

N1(C(C2=CC=CC=C2)C3=CC=CC=C3)CCN(C/C=C/C4=CC=CC=C4)CC1
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 7.14 mg/mL (19.38 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.7136 mL

13.5682 mL

27.1363 mL

5 mM

0.5427 mL

2.7136 mL

5.4273 mL

10 mM

0.2714 mL

1.3568 mL

2.7136 mL

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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 0.71 mg/mL (1.93 mM); Clear solution

This protocol yields a clear solution of ≥ 0.71 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (7.1 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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 0.71 mg/mL (1.93 mM); Clear solution

This protocol yields a clear solution of ≥ 0.71 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (7.1 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 0.71 mg/mL (1.93 mM); Clear solution

This protocol yields a clear solution of ≥ 0.71 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (7.1 mg/mL) to 900 μL Corn oil, and mix evenly.

Working Solution

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.

Protocol 1

Add each solvent one by one: 50% PEG300 50% Saline

Solubility: 12 mg/mL (32.56 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (277 KB)
SDS (540 KB)
- English - EN (540 KB)
- Français - FR (540 KB)
- Deutsch - DE (540 KB)
- Norwegian - NO (540 KB)
- Español - ES (540 KB)
- Swedish - SV (540 KB)
- Italian - IT (540 KB)
- Korean - KR (540 KB)
- Portuguese - PT (540 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Arab SF, et al. Inhibition of voltage-gated calcium currents in type II vestibular hair cells by cinnarizine. Naunyn Schmiedebergs Arch Pharmacol. 2004 Jun;369(6):570-5. [Content Brief]

[2]. Düwel P, et al. Effects of cinnarizine on calcium and pressure-dependent potassium currents in guinea pig vestibular hair cells. Naunyn Schmiedebergs Arch Pharmacol. 2005 Jun;371(6):441-8. [Content Brief]

[3]. Ng E, et al. Evaluation of Aldosterone Suppression by Cinnarizine, a Putative Cav1.3 Inhibitor. J Clin Endocrinol Metab. 2025 Feb 10:dgaf081. [Content Brief]

[4]. Serrano A, et al. Effects of cinnarizine, a calcium antagonist that produces human parkinsonism, in parkin knock out mice. Neuropharmacology. 2005 Aug;49(2):208-19. [Content Brief]

[5]. Li BQ, et al. Effect of route of administration on the pharmacokinetics and toxicokinetics of cinnarizine in dogs. Eur J Pharm Sci. 2010 Jun 14;40(3):197-201. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.7136 mL	13.5682 mL	27.1363 mL	67.8408 mL
	5 mM	0.5427 mL	2.7136 mL	5.4273 mL	13.5682 mL
	10 mM	0.2714 mL	1.3568 mL	2.7136 mL	6.7841 mL
	15 mM	0.1809 mL	0.9045 mL	1.8091 mL	4.5227 mL

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Cinnarizine

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