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Meclizine dihydrochloride

Catalog No. T1110 CAS 1104-22-9

Synonyms: Meclozine dihydrochloride, NSC28728, Meclizine 2HCl

Meclizine dihydrochloride (NSC28728) is a histamine H1 antagonist used in the treatment of motion sickness, vertigo, and nausea during pregnancy and radiation sickness.

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Meclizine dihydrochloride Chemical Structure

Meclizine dihydrochloride, CAS 1104-22-9

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Purity: 99.79%

Purity: 99.08%

Purity: 98.1%

Biological Description

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Storage & Solubility Information

Description	Meclizine dihydrochloride (NSC28728) is a histamine H1 antagonist used in the treatment of motion sickness, vertigo, and nausea during pregnancy and radiation sickness.
In vitro	Meclizine increases the expression of mouse CAR target genes in a CAR-dependent manner.
In vivo	In vitro, Meclizine exhibits dose-dependent augmentation of mCAR transactivation and enhances the recruitment of the coactivator SRC-1 (steroid receptor coactivator-1) to the receptor. Conversely, in mouse hepatocytes expressing only hCAR and not mCAR, Meclizine inhibits hCAR transcriptional activation and suppresses the expression of luminal-induced CAR downstream genes, which include CYP2B10, CYP3A11, and CYP1A2 (cytochrome P450 monooxygenases). Therefore, Meclizine acts as an agonist ligand for mouse CAR (constitutive androstane receptor) but as a reverse agonist for human CAR.
Cell Research	HepG2 cells are cultured in 24-well dishes with DMEM supplemented with 10% charcoal-stripped calf serum. Cells are transfected using calcium phosphate with 100 ng of receptor expression vectors, 300 ng of luciferase reporter plasmids, and 100 ng of pSV2-β-galactosidase as internal control of transfection efficiency. Drugs are added 12 h after transfection, and cells are incubated for an additional 24 h. The cell lysate is assayed for luciferase activity and normalized to β-galactosidase activity.(Only for Reference)

Synonyms	Meclozine dihydrochloride, NSC28728, Meclizine 2HCl
Molecular Weight	463.87
Formula	C25H27ClN2·2HCl
CAS No.	1104-22-9

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 23.2 mg/mL (50 mM)

References and Literature

1. King CT, et al. J Pharmacol Exp Ther, 1965, 147, 391-398. 2. Huang W, et al. Mol Endocrinol, 2004, 18(10), 2402-2408. 3. Gohil VM, et al. Hum Mol Genet, 2011, 20(2), 294-300.

Related compound libraries

This product is contained In the following compound libraries：

GPCR Compound Library Drug Repurposing Compound Library Anti-Neurodegenerative Disease Compound Library Anti-Cancer Approved Drug Library Inhibitor Library Anti-Cancer Drug Library FDA-Approved & Pharmacopeia Drug Library Orally Active Compound Library NO PAINS Compound Library Histamine & Melatonin Receptor-Targeted Compound Library

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Keywords

Meclizine dihydrochloride 1104-22-9 Apoptosis GPCR/G Protein Immunology/Inflammation Neuroscience Histamine Receptor sickness Meclozine dihydrochloride Inhibitor Huntington Meclozine Dihydrochloride Meclozine anti-motion NSC-28728 piperazine NSC28728 Meclizine Dihydrochloride Meclizine 2HCl NSC 28728 Meclizine antihistamine inhibit inhibitor

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