美克洛嗪 T40652

Product Introduction
Bioactivity


英文名: Meclizine

描述: Meclizine (Meclozine) (Meclozine)具有抗组胺作用，可可逆地抑制组胺与H1受体的相互作用。Meclizine 是哌嗪类H1拮抗剂的一个成员。Meclizine 是一种有效的抗运动病剂。Meclizine 可通过血脑屏障。Meclizine 是小鼠组成型雄烷受体(CAR)的激动剂配体，也是人CAR 的反向激动剂。Meclizine 可用于polyQ 毒性疾病的研究，如亨廷顿病。

体外活性: 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.

体内活性: 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.

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

溶解度: DMSO : 4.5 mg/mL (9.7 mM)


关键字: Meclizine

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相关库: FDA-Approved Drug Library | Drug Repurposing Compound Library | Anti-Neurodegenerative Disease Compound Library | FDA-Approved & Pharmacopeia Drug Library | Anti-Cancer Drug Library | Membrane Protein-targeted Compound Library | Anti-Cancer Clinical Compound Library | GPCR Compound Library | Inhibitor Library | Anti-Cancer Approved Drug Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途