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Meclizine

Meclizine

产品编号 T40652   CAS 569-65-3
别名: Meclozine

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。

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Meclizine Chemical Structure
Meclizine, CAS 569-65-3
规格 价格/CNY 货期 数量
1 mg ¥ 1,290 现货
5 mg ¥ 2,990 现货
10 mg ¥ 4,390 现货
25 mg ¥ 6,910 现货
50 mg ¥ 9,480 现货
100 mg ¥ 12,800 现货
其他形式的 Meclizine:
千万补贴 助力科研
BCA蛋白浓度测定试剂盒限时半价
重组蛋白限时优惠
产品目录号及名称: Meclizine (T40652)
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纯度: 95.16%
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生物活性
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存储 & 溶解度
参考文献
产品描述 Meclizine, also known as Meclozine, is a piperazine class H1 antagonist with antihistamine properties that inhibits the interaction of histamine at H1 receptors reversibly. It serves as an effective anti-motion sickness agent, able to cross the blood-brain barrier. Additionally, Meclizine acts as an agonist ligand for the mouse constitutive androstane receptor (CAR) and an inverse agonist for human CAR, making it useful in research on polyQ toxicity disorders, including Huntington's disease.
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.
别名 Meclozine
分子量 390.95
分子式 C25H27ClN2
CAS No. 569-65-3

存储

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

溶解度

DMSO: 4.5 mg/mL (9.7 mM)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.5579 mL 12.7894 mL 25.5787 mL 63.9468 mL
5 mM 0.5116 mL 2.5579 mL 5.1157 mL 12.7894 mL

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TargetMol Library Books参考文献

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.
Emedastine Trimipramine maleate Bilastine Cetirizine D8 Cimetidine Iodophenpropit dihydrobromide Noberastine Chlorpheniramine maleate

相关化合物库

该产品包含在如下化合物库中:
神经退行性疾病化合物库 抗癌上市药物库 抗癌临床化合物库 药物功能重定位化合物库 抑制剂库 抗癌药物库 膜蛋白靶向化合物库 GPCR靶点分子库 FDA 上市药物库 经典已知活性库

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请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。

体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

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您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

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

 

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