| Field | Specification |
|---|---|
| Target | |
| Alternative names | Meclozine dihydrochloride |
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C25H29Cl3N2 |
| Purity | |
| SMILES | |
| Form | Solid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
Meclizine dihydrochloride, also known as Meclozine dihydrochloride, is an antihistamine that reversibly inhibits the interaction of histamine at the H1 receptor and belongs to the piperazine class of H1 antagonists. It is an effective anti-motion sickness agent that crosses the blood-brain barrier and can be used for the research of polyQ toxicity disorders such as Huntington's disease. It also acts as an agonist ligand for the mouse constitutive androstane receptor (CAR) and as an inverse agonist for human CAR[1][2][3]. It is supplied as a white to off-white solid (C25H29Cl3N2, MW 463.87) at 99.94% purity.
Physical & Chemical Properties
| CAS Number | 1104-22-9 |
|---|---|
| Molecular Formula | C25H29Cl3N2 |
| Molecular Weight | 463.87 g/mol |
| Purity | 99.94% |
| Appearance | Solid |
| Color | White to off-white |
| SMILES | CC1=CC(CN2CCN(C(C3=CC=C(Cl)C=C3)C4=CC=CC=C4)CC2)=CC=C1.Cl.Cl |
| Target | H 1 Receptor |
| Signaling Pathway | GPCR/G Protein; Neuronal Signaling; Immunology/Inflammation; Apoptosis |
| Solubility | In Vitro: DMSO: ≥ 33.33 mg/mL (71.85 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) * "≥" means soluble, but saturation unknown. |
| Storage | 4°C, sealed storage, away from moisture. In solvent: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
[1]. Priti N. Patel, et al. Safety and Efficacy in the Treatment and Prevention of Motion Sickness.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with the Safety Data Sheet and your institution's chemical hygiene plan.
In Vitro
| Solvent | Solubility | Notes |
|---|---|---|
| DMSO | ≥ 33.33 mg/mL (71.85 mM) | use freshly opened DMSO (absorbed moisture lowers solubility) |
Aliquot the stock solution and store it at -80°C (up to 6 months) or -20°C (up to 1 month); sealed storage, away from moisture; avoid repeated freeze-thaw cycles.
In Vivo
Choose the formulation that suits the animal model and route of administration; percentages are volume ratios of the final working solution. Start from a clear DMSO stock (see In Vitro above), add the co-solvents one at a time in the order listed, mixing after each addition, and prepare the working solution fresh on the day of dosing. If precipitation or phase separation occurs, gentle warming or sonication can help.
Protocol 1
| Composition | 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% saline |
|---|---|
| Result | ≥ 2.5 mg/mL (5.39 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 2.5 mg/mL (saturation not determined). For 1 mL of working solution: add 100 μL DMSO stock (25.0 mg/mL) to 400 μL PEG300; then 50 μL Tween-80; then 450 μL saline to bring the volume to 1 mL. Saline: dissolve 0.9 g sodium chloride in ddH2O and make up to 100 mL. |
Protocol 2
| Composition | 10% DMSO + 90% (20% SBE-β-CD in saline) |
|---|---|
| Result | ≥ 2.5 mg/mL (5.39 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 2.5 mg/mL (saturation not determined). For 1 mL of working solution: add 100 μL DMSO stock (25.0 mg/mL) to 900 μL 20% SBE-β-CD in saline. 20% SBE-β-CD in saline: dissolve 2 g SBE-β-CD powder in 10 mL saline until clear (4°C, store up to one week). |
Protocol 3
| Composition | 10% DMSO + 90% Corn Oil |
|---|---|
| Result | ≥ 2.5 mg/mL (5.39 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 2.5 mg/mL (saturation not determined). Use with caution if continuous dosing will exceed two weeks. For 1 mL of working solution: add 100 μL DMSO stock (25.0 mg/mL) to 900 μL corn oil. |
Direct preparation of the working solution
These formulations are prepared directly, without a DMSO stock; use them promptly after preparation.
Protocol 4
| Composition | 15% Cremophor EL + 85% saline |
|---|---|
| Result | 10 mg/mL (21.56 mM); clear solution; requires sonication |
Data provided by the manufacturer.
In Vitro
Meclizine (Meclozine; 50 μM; 24 hours) dihydrochloride significantly raises cell survival in STHdhQ111/111 cells 24 h after serum removal, apparently through suppression of apoptosis as judged by caspase 3 and 7 cleavage. The rescue is dose-dependent (EC50 of 17.3 μM), with maximum efficacy corresponding to a 218% increase in survival over vehicle. Meclizine dihydrochloride protects striatal cells that express polyglutamine (polyQ)-expanded huntingtin against serum withdrawal-induced apoptosis in both mutant (STHdhQ111/111) and wild-type (STHdhQ7/7) striatal cells[2].
Cell Viability Assay[2]
| Cell Line | The murine striatal cells expressing wild-type (STHdhQ7/7) or mutant (STHdhQ111/111) huntingtin protein |
|---|---|
| Concentration | 50 μM |
| Incubation Time | 24 hours |
| Result | Significantly increased cell survival in STHdhQ111/111 cells at 24 h after the removal of serum. |
Western Blot Analysis[2]
| Cell Line | Mutant (STHdhQ111/111) and wild-type (STHdhQ7/7) striatal cells |
|---|---|
| Concentration | 50 μM |
| Incubation Time | 0, 4, 10, 24 hours |
| Result | Suppressed apoptosis, based on caspase 3 and 7 cleavage. |
In Vivo
Meclizine (Meclozine; 10-100 mg/kg; ip) dihydrochloride protects mice against kidney ischemia. Pretreatment with Meclizine at 100 mg/kg, 17 or 24 h before ischemia, protects the kidney in mice. Meclizine dihydrochloride lowers mitochondrial oxygen consumption through direct inhibition of the Kennedy pathway of phosphatidylethanolamine biosynthesis and up-regulates glycolysis[4].
| Animal Model | 8-10 wk old male C57BL/6 mice[4] |
|---|---|
| Dosage | 10, 30, 60 or 100 mg/kg |
| Administration | Administered intraperitoneally |
| Result | Protected mice from kidney ischemia-reperfusion injury. |
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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Ergothioneine alleviates hepatic steatosis by modulating PCYT2 to restore the phosphatidylethanolamine-ACOT8 homeostasis. Phytomedicine 2026 Aug:158:158238. PMID: 42275877
Meclizine Improves Endometrial Repair and Reduces Simulated Menstrual Bleeding in Mice with Induced Adenomyosis. Am J Obstet Gynecol 2024 Jul;231(1):113.e1-113.e13. PMID: 38367751
PFKFB3 downregulation aggravates Angiotensin II-induced podocyte detachment. Ren Fail 2023 Dec;45(1):2230318. PMID: 37427767
Dihydroartemisinin Suppresses LOXL2-Mediated Glycerophospholipid Metabolic Reprogramming to Induce Cuproptosis in Colorectal Cancer Cells. J Biochem Mol Toxicol 2025 Aug;39(8):e70420. PMID: 40746272
Wnt inhibitory factor 1 inhibits glycolysis through the HIF1α/PFKFB3 signalling pathway to regulate macrophage polarization and alleviate diabetic retinopathy. Diabet Med 2026 May;43(5):e70285. PMID: 41814504
