| Name | Meclizine dihydrochloride |
| Description | Meclizine dihydrochloride (NSC28728) is a histamine H1 antagonist used in the treatment of motion sickness, vertigo, and nausea during pregnancy and radiation sickness. |
| 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) |
| 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. |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 15 mg/mL (32.34 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (4.31 mM), Sonication is recommended.
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| Keywords | sickness | piperazine | NSC-28728 | NSC 28728 | Meclozine Dihydrochloride | Meclozine | Meclizine dihydrochloride | Meclizine | Inhibitor | inhibit | Huntington | HistamineReceptor | Histamine Receptor | H1 receptor | Apoptosis | anti-motion | antihistamine |
| Inhibitors Related | Stavudine | Aceglutamide | Urea | Tamoxifen | Cysteamine hydrochloride | Metronidazole | Citric Acid Triammonium | Formamide | Dimethyl phthalate | Alginic acid | Sodium Molybdate | Sildenafil citrate |
| Related Compound Libraries | Anti-Neurodegenerative Disease Compound Library | Pain-Related Compound Library | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Drug Repurposing Compound Library | Inhibitor Library | Anti-Cancer Approved Drug Library | FDA-Approved Drug Library | Immunology/Inflammation Compound Library | Bioactive Compounds Library Max | GPCR Compound Library | Anti-Cancer Drug Library |
United States
