Meclizine
Based on 5 publication(s) in Google Scholar
Meclizine (Meclozine), an antihistamine, reversibly inhibits the interaction of histamine at the H1 receptors. Meclizine is a member of the piperazine class of H1 antagonists. Meclizine is an effective anti-motion sickness agent. Meclizine crosses the blood–brain barrier. Meclizine is an agonist ligand for mouse constitutive androstane receptor (CAR) and an inverse agonist for Human CAR. Meclizine can be used for the research of polyQ toxicity disorders, such as Huntington's disease.
For research use only. We do not sell to patients.
- CAS No.: 569-65-3
- Formula: C25H27ClN2
- Molecular Weight:390.95
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications Citing Use of MedChemExpress (MCE) Meclizine
MoreAll Histamine Receptor Isoforms
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Biological Activity
Description
IC50 & Target
[1]|
H1 Receptor |
In Vitro
Meclizine (Meclozine; 50 μM; 24 hours) significantly increases cell survival in STHdh cells at 24 h after the removal of serum, evidently by suppressing apoptosis, based on caspase 3 and 7 cleavage. The rescue is dose-dependent with an EC50 of 17.3 μm, and a maximum efficacy of 218% increased survival over vehicle. Meclizine protects striatal cells expressing polyglutamine (polyQ)-expanded huntingtin from serum withdrawal-induced apoptosis of mutant (STHdhQ111/111) and wild-type (STHdhQ7/7) striatal cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:The murine striatal cells expressing wild-type (STHdhQ7/7) or mutant (STHdhQ111/111) huntingtin protein
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Concentration:50 µM
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Incubation Time:24 hours
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Result:Significantly increased cell survival in STHdhQ111/111 cells at 24 h after the removal of serum.
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Cell Line:Mutant (STHdhQ111/111) and wild-type (STHdhQ7/7) striatal cells
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Concentration:50 µM
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Incubation Time:0, 4, 10, 24 hours
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Result:Suppressed apoptosis, based on caspase 3 and 7 cleavage.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:8-10 wk old male C57BL/6 mice[4]
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Dosage:10, 30, 60 or 100 mg/kg
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Administration:Administered intraperitoneally
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Result:Protected mice from kidney ischemia-reperfusion injury.
Chemical Information
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CAS No. 569-65-3
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Molecular Weight 390.95
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Formula C25H27ClN2
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SMILES
CC1=CC(CN2CCN(C(C3=CC=C(Cl)C=C3)C4=CC=CC=C4)CC2)=CC=C1
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Synonyms
Meclozine
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (5)
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Journal Impact Factor
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Most Recent
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Phytomedicine
Ergothioneine alleviates hepatic steatosis by modulating PCYT2 to restore the phosphatidylethanolamine-ACOT8 homeostasis. [Abstract]2026 Aug:158:158238. PMID: 42275877 -
Am J Obstet Gynecol
Meclizine Improves Endometrial Repair and Reduces Simulated Menstrual Bleeding in Mice with Induced Adenomyosis. [Abstract]2024 Jul;231(1):113.e1-113.e13. PMID: 38367751 -
Ren Fail
2023 Dec;45(1):2230318. PMID: 37427767 -
J Biochem Mol Toxicol
Dihydroartemisinin Suppresses LOXL2-Mediated Glycerophospholipid Metabolic Reprogramming to Induce Cuproptosis in Colorectal Cancer Cells. [Abstract]2025 Aug;39(8):e70420. PMID: 40746272 -
Diabet Med
Wnt inhibitory factor 1 inhibits glycolysis through the HIF1α/PFKFB3 signalling pathway to regulate macrophage polarization and alleviate diabetic retinopathy. [Abstract]2026 May;43(5):e70285. PMID: 41814504
Solvent & Solubility
In Vitro:
DMSO : 100 mg/mL (255.79 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 5 mg/mL (12.79 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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: ≥ 5 mg/mL (12.79 mM); Suspended solution
This protocol yields a suspended solution of ≥ 5 mg/mL (saturation unknown). Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.
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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%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.
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
References
[1]. Priti N. Patel, et al. Safety and Efficacy in the Treatment and Prevention of Motion Sickness.
[2]. Vishal M Gohil, et al. Meclizine is neuroprotective in models of Huntington's disease. Hum Mol Genet. 2011 Jan 15;20(2):294-300. [Content Brief]
[3]. Wendong Huang, et al. Meclizine Is an Agonist Ligand for Mouse Constitutive Androstane Receptor (CAR) and an Inverse Agonist for Human CAR [Content Brief]
[4]. Seiji Kishi, et al. Meclizine Preconditioning Protects the Kidney Against Ischemia-Reperfusion Injury. EBioMedicine. 2015 Jul 29;2(9):1090-101. [Content Brief]
Complete Stock Solution Preparation Table
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.5579 mL | 12.7894 mL | 25.5787 mL | 63.9468 mL |
| 5 mM | 0.5116 mL | 2.5579 mL | 5.1157 mL | 12.7894 mL | |
| 10 mM | 0.2558 mL | 1.2789 mL | 2.5579 mL | 6.3947 mL | |
| 15 mM | 0.1705 mL | 0.8526 mL | 1.7052 mL | 4.2631 mL | |
| 20 mM | 0.1279 mL | 0.6395 mL | 1.2789 mL | 3.1973 mL | |
| 25 mM | 0.1023 mL | 0.5116 mL | 1.0231 mL | 2.5579 mL | |
| 30 mM | 0.0853 mL | 0.4263 mL | 0.8526 mL | 2.1316 mL | |
| 40 mM | 0.0639 mL | 0.3197 mL | 0.6395 mL | 1.5987 mL | |
| 50 mM | 0.0512 mL | 0.2558 mL | 0.5116 mL | 1.2789 mL | |
| 60 mM | 0.0426 mL | 0.2132 mL | 0.4263 mL | 1.0658 mL | |
| 80 mM | 0.0320 mL | 0.1599 mL | 0.3197 mL | 0.7993 mL | |
| 100 mM | 0.0256 mL | 0.1279 mL | 0.2558 mL | 0.6395 mL |