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Meclizine 2HCl Histamine Receptor antagonist

Name: Meclizine 2HCl
Brand: Selleck Chemicals
SKU: S1986
Availability: InStock
Rating: 5 (3 reviews)

Cat.No.S1986

Meclizine (NSC 28728,Meclozine dihydrochloride) is a histamine H1 receptor antagonist used to treat nausea and motion sickness, has anti-histamine, anti-muscarinic and anti-oxidative phosphorylation properties, also an agonist ligand for mCAR (constitutive androstane receptor) and an inverse agonist for hCAR.

Chemical Structure

Molecular Weight: 463.87

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Quality Control

Batch: Purity: 99.98%

99.98

Related Targets	Adrenergic Receptor AChR 5-HT Receptor COX Calcium Channel Dopamine Receptor GABA Receptor TRP Channel Cholinesterase (ChE) GluR
Other Histamine Receptor Inhibitors	GSK2879552 Dihydrochloride JNJ-7777120 Mianserin HCl Ebastine Astemizole Ciproxifan Maleate Rupatadine Lafutidine Cloperastine hydrochloride Mizolastine

Solubility

In vitro
Batch:

Ethanol : 2 mg/mL

DMSO : 1 mg/mL (2.15 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	10.000mg/ml (21.56mM)	Taking the 1 mL working solution as an example, add 50 μL of 200 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

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Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	463.87	Formula	C₂₅H₂₇Cl₂N₂.2HCl	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	1104-22-9	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	NSC 28728,Meclozine dihydrochloride			SMILES	CC1=CC(=CC=C1)CN2CCN(CC2)C(C3=CC=CC=C3)C4=CC=C(C=C4)Cl.Cl.Cl

Read more about storage stability stock solution CAS number SMILES

Mechanism of Action

Targets/IC₅₀/Ki	Histamine H1 receptor
In vitro	Meclizine is a histamine H1 receptor antagonist used to treat nausea and motion sickness, possesses anticholinergic, central nervous system depressant, and local anesthetic effects. Meclizine is an agonist ligand for mouse CAR (constitutive androstane receptor), and an inverse agonist for human CAR. Meclizine increases mCAR transactivation in a dose-dependent manner, stimulates binding of steroid receptor coactivator 1 to the murine receptor in vitro. In contrast, meclizine suppresses hCAR transactivation and inhibits the phenobarbital-induced expression of the CAR target genes, cytochrome p450 monooxygenase (CYP)2B10, CYP3A11, and CYP1A2, in primary hepatocytes derived from mice expressing hCAR, but not mCAR.
In vivo	Meclizine administration to mice increases expression of CAR target genes in a CAR-dependent manner. Meclizine silence oxidative metabolism, suppresses apoptotic cell death in a murine cellular model of polyglutamine (polyQ) toxicity.
References	[1] https://pubmed.ncbi.nlm.nih.gov/14269616/ [2] https://pubmed.ncbi.nlm.nih.gov/15272053/ [3] https://pubmed.ncbi.nlm.nih.gov/20977989/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2026-07-02)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT07681076	NOT_YET_RECRUITING	Healthy Volunteers	Karuna Therapeutics, Inc., a Bristol Myers Squibb company	2026-08-03	PHASE4
NCT05852730	RECRUITING	Motion Sickness, Space; Motion Simulation; Parabolic Flight	Repurposed Therapeutics, Inc.	2021-08-10	PHASE2
NCT03253289	COMPLETED	Carcinoma, Hepatocellular	Tannaz Armaghnay	2017-10-13	PHASE1
NCT04482985	UNKNOWN	Seasickness; Meclizine	Medical Corps, Israel Defense Force	2020-09-01	PHASE4
NCT04564144	UNKNOWN	Emesis	Mansoura University	2020-06-01	PHASE1; PHASE2
NCT04482985	Unknown status	Seasickness\|Meclizine	Medical Corps Israel Defense Force	2020-09-01	Phase 4

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