Powder: -20°C for 3 years
In solvent: -80°C for 2 years
Meclizine (Meclozine) shows antihistamine activity and reversibly inhibits the interaction of histamine at the H1 receptors . Meclizine is a member of the piperazine class of H1 antagonists. Meclizine is an effective anti-motion sickness agent. Meclizine crosses the blood–brain barrier. Meclizine is an agonist ligand for mouse constitutive androstane receptor (CAR) and an inverse agonist for Human CAR. Meclizine can be used for the research of polyQ toxicity disorders, such as Huntington's disease.
Description | Meclizine (Meclozine) shows antihistamine activity and reversibly inhibits the interaction of histamine at the H1 receptors . Meclizine is a member of the piperazine class of H1 antagonists. Meclizine is an effective anti-motion sickness agent. Meclizine crosses the blood–brain barrier. Meclizine is an agonist ligand for mouse constitutive androstane receptor (CAR) and an inverse agonist for Human CAR. Meclizine can be used for the research of polyQ toxicity disorders, such as Huntington's disease. |
Targets&IC50 | Hepsin:2.02 μM, Homo sapiens:1.2 μM, Leishmania promastigotes:17.3 μM-35.11 μM |
In vitro | Meclizine (Meclozine; 50 μM; 24 hours) significantly increases cell survival in ST Hdh cells at 24 h after the removal of serum, evidently by suppressing apoptosis, based on caspase 3 and 7 cleavage. The rescue is dose-dependent with an EC 50 of 17.3 μm, and a maximum efficacy of 218% increased survival over vehicle. Meclizine protects striatal cells expressing polyglutamine (polyQ)-expanded huntingtin from serum withdrawal-induced apoptosis of mutant (ST HdhQ111/111 ) and wild-type (ST HdhQ7/7 ) striatal cells [2] . Cell Viability Assay [2] Cell Line: The murine striatal cells expressing wild-type (ST HdhQ7/7 ) or mutant (ST HdhQ111/111 ) huntingtin protein Concentration: 50 μM Incubation Time: 24 hours Result: Significantly increased cell survival in ST HdhQ111/111 cells at 24 h after the removal of serum. Western Blot Analysis [2] Cell Line: Mutant (ST HdhQ111/111 ) and wild-type (ST HdhQ7/7 ) striatal cells Concentration: 50 μM Incubation Time: 0, 4, 10, 24 hours Result: Suppressed apoptosis, based on caspase 3 and 7 cleavage. |
In vivo | Meclizine (Meclozine; 10-100 mg/kg; ip) protects mouse against kidney ischemia. Pretreatment with 100 mg/kg of Meclizine, 17 or 24 h prior to ischemia shows kidney protection in mice. Meclizine reduces mitochondrial oxygen consumption by directly inhibiting the Kennedy pathway of phosphatidylethanolamine biosynthesis and up-regulated glycolysis [4] . Animal Model: 8-10 wk old male C57BL/6 mice [4] Dosage: 10, 30, 60 or 100 mg/kg Administration: Administered intraperitoneally Result: Protected mice from kidney ischemia-reperfusion injury. |
Synonyms | Meclozine |
Molecular Weight | 390.95 |
Formula | C25H27ClN2 |
CAS No. | 569-65-3 |
Powder: -20°C for 3 years
In solvent: -80°C for 2 years
DMSO: 4.5 mg/mL (9.7 mM)
( < 1 mg/ml refers to the product slightly soluble or insoluble )
You can also refer to dose conversion for different animals. More
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Meclizine 569-65-3 GPCR/G Protein Immunology/Inflammation Neuroscience Histamine Receptor Meclozine Inhibitor inhibitor inhibit