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Meclizine

Catalog No. T40652 CAS 569-65-3

Synonyms: Meclozine

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.

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Meclizine, CAS 569-65-3

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Purity: 98%

Biological Description

Chemical Properties

Storage & Solubility Information

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

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

DMSO: 4.5 mg/mL (9.7 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

1. Priti N. Patel, et al. Safety and Efficacy in the Treatment and Prevention of Motion Sickness. Clinical Medicine Insights: Therapeutics. 2011;3. 2. Vishal M Gohil, et al. Meclizine is neuroprotective in models of Huntington's disease. Hum Mol Genet. 2011 Jan 15;20(2):294-300. 3. Wendong Huang, et al. Meclizine Is an Agonist Ligand for Mouse Constitutive Androstane Receptor (CAR) and an Inverse Agonist for Human CAR.Mol Endocrinol. 2004 Oct;18(10):2402-8. 4. Seiji Kishi, et al. Meclizine Preconditioning Protects the Kidney Against Ischemia-Reperfusion Injury. EBioMedicine. 2015 Jul 29;2(9):1090-101.

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Keywords

Meclizine 569-65-3 GPCR/G Protein Immunology/Inflammation Neuroscience Histamine Receptor Meclozine Inhibitor inhibitor inhibit

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