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Meclizine dihydrochloride
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Meclizine dihydrochloride图片
CAS NO:1104-22-9
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
100mg电议
5 g电议
10 g电议
50 g电议

产品名称
盐酸美克洛嗪
Meclozine dihydrochloride
产品介绍
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。
生物活性

Meclizine (Meclozine) dihydrochloride, anantihistamine, reversibly inhibits the interaction of histamine at theH1 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 mouseconstitutive androstane receptor (CAR)and an inverse agonist for Human CAR[1][2][3].

IC50& Target[1]

H1Receptor

 

体外研究
(In Vitro)

Meclizine (Meclozine; 50 μM; 24 hours) dihydrochloride significantly increases cell survival in STHdhQ111/111cells 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 EC50of 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].

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 STHdhQ111/111cells 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].

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

性状

Solid

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 : ≥ 33.33 mg/mL(71.85 mM)

*"≥" means soluble, but saturation unknown.

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM2.1558 mL10.7789 mL21.5578 mL
5 mM0.4312 mL2.1558 mL4.3116 mL
10 mM0.2156 mL1.0779 mL2.1558 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℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 15% Cremophor EL    85% Saline

    Solubility: 10 mg/mL (21.56 mM); Clear solution; Need ultrasonic

  • 2.

    请依序添加每种溶剂: Cremophor EL

    Solubility: 5 mg/mL (10.78 mM); Clear solution; Need ultrasonic and warming

  • 3.

    请依序添加每种溶剂: 10% DMSO    40%PEG300   5%Tween-80   45% saline

    Solubility: ≥ 2.5 mg/mL (5.39 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.39 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH2O 中,得到澄清透明的生理盐水溶液
  • 4.

    请依序添加每种溶剂: 10% DMSO    90% (20%SBE-β-CDin saline)

    Solubility: ≥ 2.5 mg/mL (5.39 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.39 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 5.

    请依序添加每种溶剂: 10% DMSO    90%corn oil

    Solubility: ≥ 2.5 mg/mL (5.39 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.39 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在本网站选购。