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Pack Size | Price | Availability | Quantity |
---|---|---|---|
100 mg | $50 | In Stock |
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) |
Alias | 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 | Shipping with blue ice. | |||||||||||||||||||||||||
Solubility Information | DMSO: 15 mg/mL (32.34 mM), Sonication is recommended. ![]() | |||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||
DMSO
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