Meclizine dihydrochloride

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Description: Human pregnane X receptor agonist; H1 antagonist
Alternative Names: Meclozine
Chemical Name: 1-[(4-Chlorophenyl)phenylmethyl]4-[(3-methylphenyl)methyl]piperazine dihydrochloride
Purity: ≥99% (HPLC)
Datasheet
Citations (2)
Reviews
Literature (1)

Biological Activity for Meclizine dihydrochloride

Meclizine dihydrochloride is a human pregnane X receptor (hPXR) agonist; it is a more potent activator of hPXR than rat PXR. Meclizine increases hPXR target gene expression in human hepatocyte primary cultures. It also acts as a histamine H1 receptor antagonist. Meclizine attenuates mitochondrial respiration and increases glycolysis. The product inhibits rotenone-induced cell death in stem cell-derived dopaminergic neuronal culture and confers neuroprotection in models of polyglutamine (polyQ) toxicity.

Compound Libraries for Meclizine dihydrochloride

Meclizine dihydrochloride is also offered as part of the Tocriscreen FDA-Approved Drugs. Find out more about compound libraries available from Tocris.

Technical Data for Meclizine dihydrochloride

M. Wt 463.87
Formula C25H27ClN2.2HCl
Storage Desiccate at RT
Purity ≥99% (HPLC)
CAS Number 1104-22-9
PubChem ID 64713
InChI Key VCTHNOIYJIXQLV-UHFFFAOYSA-N
Smiles CC1=CC(CN(CC4)CCN4C(C3=CC=C(Cl)C=C3)C2=CC=CC=C2)=CC=C1.Cl.Cl

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for Meclizine dihydrochloride

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 23.19 50

Preparing Stock Solutions for Meclizine dihydrochloride

The following data is based on the product molecular weight 463.87. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
0.5 mM 4.31 mL 21.56 mL 43.12 mL
2.5 mM 0.86 mL 4.31 mL 8.62 mL
5 mM 0.43 mL 2.16 mL 4.31 mL
25 mM 0.09 mL 0.43 mL 0.86 mL

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Product Datasheets for Meclizine dihydrochloride

References for Meclizine dihydrochloride

References are publications that support the biological activity of the product.

Parada et al (2001) The major role of peripheral release of histamine and 5-hydroxytryptamine in formalin-induced nociception. Neuroscience 102 937 PMID: 11182255

Gohil et al (2010) Meclizine is neuroprotective in models of Huntington's disease. Hum.Mol.Genet. 20 294 PMID: 20977989

Lau et al (2011) Differential effect of meclizine on the activity of human pregnane X receptor and constitutive androstane receptor. J.Pharmacol.Exp.Ther. 336 816 PMID: 21131266

Oosterveen et al (2021) Pluripotent stem cell derived dopaminergic subpopulations model the selective neuron degeneration in Parkinson's disease. Stem Cell Reports PMID: 34678205


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View Related Products by Product Action

View all Pregnane X Receptor Agonists

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2 Citations for Meclizine dihydrochloride

Citations are publications that use Tocris products. Selected citations for Meclizine dihydrochloride include:

Hong et al (2016) Meclizine-induced enhanced glycolysis is neuroprotective in Parkinson disease cell models. Sci Rep 6 25344 PMID: 27145922

Oosterveen et al (2021) Pluripotent stem cell derived dopaminergic subpopulations model the selective neuron degeneration in Parkinson's disease. Stem Cell Reports 16 2718 PMID: 34678205


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Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

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Retinoid Receptors Scientific Review

Retinoid Receptors Scientific Review

Written by Alexander Moise, this review summarizes the nature of retinoid receptors, their isotype and isoform variants and modulation of retinoid signaling. Compounds available from Tocris are listed.