2. Membrane Transporter/Ion Channel Neuronal Signaling Immunology/Inflammation GPCR/G Protein
  3. Calcium Channel Histamine Receptor
  4. Cinnarizine

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.

For research use only. We do not sell to patients.

Cinnarizine Chemical Structure

Cinnarizine Chemical Structure

CAS No. : 298-57-7

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Solution
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Solid
500 mg In-stock
1 g In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Cinnarizine:

Cinnarizine Related Antibodies

Top Publications Citing Use of Products

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N-type calcium channel L-type calcium channel P/Q-type calcium channel T-type calcium channel Calcium Channel

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H1 Receptor H2 Receptor H3 Receptor H4 Receptor Histamine Receptor

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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[1][2][3][4][5].

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 (ICa) 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.

Cinnarizine Related Antibodies

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
Molecular Weight

368.51

Formula

C26H28N2
CAS No.
Appearance

Solid

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.7136 mL 13.5682 mL 27.1363 mL
5 mM 0.5427 mL 2.7136 mL 5.4273 mL
View the 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, 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.

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  • Dilution Calculator

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

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo:

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.

  • 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.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • 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.

    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.

  • 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:

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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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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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

Purity: 99.63%

SDS (537 KB)

COA (246 KB) HNMR (259 KB) LCMS (94 KB)

Handling Instructions (2659 KB)
References

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, 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 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Cinnarizine298-57-7Calcium ChannelHistamine ReceptorCa2+ channelsCa channelsInhibitorinhibitorinhibit

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