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盐酸美克洛嗪 /Meclizine dihydrochloride {[allProObj[0].p_purity_real_show]}

货号:A142777 同义名: 美克洛嗪二盐酸盐 / Meclozine dihydrochloride;Meclizine (hydrochloride)

Meclizine 2HCl is a histamine H1 receptor antagonist with Ki of 250 nM and is used to treat nausea and motion sickness.

Meclizine dihydrochloride 化学结构 CAS号:1104-22-9
Meclizine dihydrochloride 化学结构
CAS号:1104-22-9
Meclizine dihydrochloride 3D分子结构
CAS号:1104-22-9
Meclizine dihydrochloride 化学结构 CAS号:1104-22-9
Meclizine dihydrochloride 3D分子结构 CAS号:1104-22-9
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Meclizine dihydrochloride 纯度/质量文件 产品仅供科研

货号:A142777 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 H1 receptor H2 receptor H3 receptor H4 receptor Histamine receptor 其他靶点 纯度
Hydroxyzine 2HCl 99+%
Cyclizine 97%
Loratadine +

B(0)AT2, IC50: 4 μM

98%
Desloratadine ++

Histamine H1 receptor, IC50: 51 nM

98%
Doxylamine succinate 99%
Ebastine 98%
Tripelennamine HCl +

H1 receptor, IC50: 30 μM

98%
Meclizine dihydrochloride 98%
Chlorpheniramine maleate +++

Histamine H1 receptor, IC50: 12 nM

99%
Diphenhydramine HCl 99%
Alcaftadine ++++

H1 receptor, pKi: 8.5

++

H2 receptor, pKi: 7.2

99%+
Fexofenadine HCl ++

Histamine H1 receptor, IC50: 246 nM

99%+
Bilastine +++

H1 receptor, Ki: 44.15 nM

98%
Pemirolast potassium 98%
Bepotastine besilate +

Histamine H1 receptor, pIC50: 5.7

98%
Mizolastine +++

Histamine H1 receptor, IC50: 47 nM

98%
Brompheniramine maleate 98%
Carbinoxamine maleate salt 99+%
Clemastine fumarate ++++

Histamine H1 receptor, IC50: 3 nM

98%
Ketotifen fumarate salt 95%
Rupatadine Fumarate ++

Histamine H1 receptor, Ki: 102 nM

PAFR 98%
Famotidine 97%
Roxatidine Acetate HCl +

Histamine H2 receptor, IC50: 3.2 μM

98%
Lafutidine 99%
Cimetidine 98%
Nizatidine ++++

Histamine H2 receptor, IC50: 0.9 nM

AChE 98%
Ranitidine 98%
Betahistine +

Histamine H3 receptor, IC50: 1.9 μM

98%
Ciproxifan maleate +++

Histamine H3 receptor, IC50: 9.2 nM

99%+
S 38093 ++

rat H3 receptor, Ki: 1.44 μM

human H3 receptor, Ki: 1.2 μM

98%
JNJ-7777120 ++++

Histamine H4 receptor, Ki: 4.5 nM

98%
Azelastine HCl 98%
Epinastine HCl 98%
Levodropropizine 97%
Cyproheptadine hydrochloride 98%
Hesperetin 97%
Olopatadine HCl 98%
Mianserin hydrochloride 99+%
Buclizine 2HCl 97%
Latrepirdine 2HCl GluR 98%
Cetirizine 2HCl 98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

Meclizine dihydrochloride 生物活性

靶点
  • H1 receptor

描述 Meclizine dihydrochloride, is a piperazine-derived histamine H1 antagonist, and has been frequently used for prevention and treatment of vomiting and nausea. In primary bone marrow-derived macrophages (BMMs), meclizine reduced osteoclast formation and bone resorption in a dose-dependent manner[3]. Meclizine is also an agonist of human pregnane X receptor (PXR). The inhibition of human liver microsomal testosterone 6β-hydroxylation by meclizine occurred by a mixed mode and with an apparent Ki of 31 ± 6μM[4]. Meclizine is a first generation antihistamine that is used largely to treat vertigo and motion sickness. It has not been linked to instances of clinically apparent acute liver injury[5]. Meclizine protected against 6-hydroxydopamine-induced apoptosis and cell death in both SH-SY5Y cells and rat primary cortical cultures. It increases the level of 6-phosphofructo-2-kinase/fructose-2,6-biphosphatase 3 (PFKFB3), which activates phosphofructokinase, a rate-determining enzyme of glycolysis[6].

Meclizine dihydrochloride 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT02625181 Postoperative Nausea and Vomit... 展开 >>ing 收起 << Not Applicable Completed - United States, Tennessee ... 展开 >> Vanderbilt University Medical Center Nashville, Tennessee, United States, 37212 收起 <<
NCT02130622 - Terminated(Lack of recruitment... 展开 >>) 收起 << - -
NCT02130622 Diabetic Gastroparesis Phase 2 Terminated(Lack of recruitment... 展开 >>) 收起 << - United States, New Hampshire ... 展开 >> Dartmouth-Hitchcock Medical Center Lebanon, New Hampshire, United States, 03756 收起 <<

Meclizine dihydrochloride 参考文献

[1]Huang W, Zhang J, 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.

[2]King CT, Weaver SA, Narrod SA. Antihistamine and Teratogenicity in the Rat. J Pharmacol Exp Ther. 1965 Mar;147:391-8.

[3]Guo J, Li W, Wu Y, Jing X, Huang J, Zhang J, Xiang W, Ren R, Lv Z, Xiao J, Guo F. Meclizine Prevents Ovariectomy-Induced Bone Loss and Inhibits Osteoclastogenesis Partially by Upregulating PXR. Front Pharmacol. 2017 Oct 4;8:693

[4]Foo WY, Tay HY, Chan EC, Lau AJ. Meclizine, a pregnane X receptor agonist, is a direct inhibitor and mechanism-based inactivator of human cytochrome P450 3A. Biochem Pharmacol. 2015 Oct 1;97(3):320-30

[5]LiverTox: Clinical and Research Information on Drug-Induced Liver Injury [Internet]. Bethesda (MD): National Institute of Diabetes and Digestive and Kidney Diseases; 2012–. Meclizine. 2017 Jan 16

[6]Hong CT, Chau KY, Schapira AH. Meclizine-induced enhanced glycolysis is neuroprotective in Parkinson disease cell models. Sci Rep. 2016 May 5;6:25344

Meclizine dihydrochloride 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.16mL

0.43mL

0.22mL

10.78mL

2.16mL

1.08mL

21.56mL

4.31mL

2.16mL

Meclizine dihydrochloride 技术信息

CAS号1104-22-9
分子式C25H29Cl3N2
分子量 463.87
别名 美克洛嗪二盐酸盐 ;Meclozine dihydrochloride;Meclizine (hydrochloride);NSC 28728;Meclozine;Meclizine 2HCl
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Inert atmosphere,Room Temperature

溶解度

DMSO: 35 mg/mL(75.45 mM),注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方
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