Meclizine dihydrochloride(Synonyms: 盐酸美克洛嗪; Meclozine dihydrochloride)

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Meclizine dihydrochloride (Synonyms: 盐酸美克洛嗪; Meclozine dihydrochloride) 纯度: 99.95%

Meclizine (Meclozine) dihydrochloride 是一种抗组胺剂 (antihistamine)，可逆地抑制组胺与 H1 受体的相互作用。Meclizine dihydrochloride 是哌嗪类 H1 拮抗剂。Meclizine dihydrochloride 是一种有效的抗晕车剂。Meclizine dihydrochloride 可透过血脑屏障，可用于多聚谷氨酰胺毒性障碍（例如亨廷顿舞蹈症）方面的研究。Meclizine dihydrochloride 是小鼠组成型雄甾烷受体 (CAR) 激动剂，是人 CAR 的反向激动剂。

Meclizine dihydrochloride(Synonyms: 盐酸美克洛嗪; Meclozine dihydrochloride)

Meclizine dihydrochloride Chemical Structure

CAS No. : 1104-22-9

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥550 In-stock
100 mg ￥500 In-stock
5 g ￥950 In-stock
10 g   询价  
50 g   询价  

* Please select Quantity before adding items.

生物活性

Meclizine (Meclozine) dihydrochloride, an antihistamine, reversibly inhibits the interaction of histamine at the H1 receptors. Meclizine dihydrochloride is a member of the piperazine class of H1 antagonists. Meclizine dihydrochloride is an effective anti-motion sickness agent. Meclizine dihydrochloride crosses the blood-brain barrier. Meclizine dihydrochloride can be used for the research of polyQ toxicity disorders, such as Huntington’s disease. Meclizine dihydrochloride is an agonist ligand for mouse constitutive androstane receptor (CAR) and an inverse agonist for Human CAR[1][2][3].

IC50 & Target[1]

H1 Receptor

 

体外研究
(In Vitro)

Meclizine (Meclozine; 50 µM; 24 hours) dihydrochloride significantly increases cell survival in STHdhQ111/111 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 EC50 of 17.3 µm, and a maximum efficacy of 218% increased survival over vehicle. Meclizine dihydrochloride protects striatal cells expressing polyglutamine (polyQ)-expanded huntingtin from serum withdrawal-induced apoptosis of mutant (STHdhQ111/111) and wild-type (STHdhQ7/7) striatal cells[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[2]

Cell Line: The murine striatal cells expressing wild-type (STHdhQ7/7) or mutant (STHdhQ111/111) huntingtin protein
Concentration: 50 µM
Incubation Time: 24 hours
Result: Significantly increased cell survival in STHdhQ111/111 cells at 24 h after the removal of serum.

Western Blot Analysis[2]

Cell Line: Mutant (STHdhQ111/111) and wild-type (STHdhQ7/7) striatal cells
Concentration: 50 µM
Incubation Time: 0, 4, 10, 24 hours
Result: Suppressed apoptosis, based on caspase 3 and 7 cleavage.

体内研究
(In Vivo)

Meclizine (Meclozine; 10-100 mg/kg; ip) dihydrochloride 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 dihydrochloride reduces mitochondrial oxygen consumption by directly inhibiting the Kennedy pathway of phosphatidylethanolamine biosynthesis and up-regulated glycolysis[4].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

分子量

463.87

Formula

C25H29Cl3N2
CAS 号

1104-22-9
中文名称

盐酸美克洛嗪
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
溶解性数据
In Vitro: 

DMSO : 92 mg/mL (198.33 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.1558 mL 10.7789 mL 21.5578 mL
5 mM 0.4312 mL 2.1558 mL 4.3116 mL
10 mM 0.2156 mL 1.0779 mL 2.1558 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
参考文献

  • [1]. Priti N. Patel, et al. Safety and Efficacy in the Treatment and Prevention of Motion Sickness.

    [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

    [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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