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Meclizine dihydrochloride monohydrate
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 monohydrate图片
CAS NO:31884-77-2
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品名称
盐酸美克洛嗪一水合物
Meclozine dihydrochloride monohydrate
产品介绍
Meclizine (Meclozine) dihydrochloride monohydrate 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 monohydrate 是哌嗪类 H1 拮抗剂,也是一种有效的抗晕车剂。Meclizine dihydrochloride monohydrate 可透过血脑屏障。Meclizine dihydrochloride monohydrate 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 monohydrate 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。
生物活性

Meclizine (Meclozine) dihydrochloride monohydrate, anantihistamine, reversibly inhibits the interaction of histamine at theH1 receptors. Meclizine dihydrochloride is a member of the piperazine class of H1 antagonists. Meclizine dihydrochloride monohydrate is an effective anti-motion sickness agent. Meclizine dihydrochloride monohydrate crosses the blood-brain barrier. Meclizine dihydrochloride monohydrate is an agonist ligand for mouseconstitutive androstane receptor (CAR)and an inverse agonist for Human CAR. Meclizine dihydrochloride monohydrate can be used for the research of polyQ toxicity disorders, such as Huntington's disease[1][2][3].

IC50& Target[1]

H1Receptor

 

体外研究
(In Vitro)

Meclizine (Meclozine; 50 μM; 24 hours) dihydrochloride monohydrate 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 monohydrate 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 monohydrate 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 monohydrate 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

481.89

Formula

C25H31Cl3N2O

CAS 号

31884-77-2

中文名称

盐酸美克洛嗪一水合物

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.