Clemastine fumarate | HS-592 fumarate | Histamine Receptor

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富马酸氯马斯汀 /Clemastine fumarate {[allProObj[0].p_purity_real_show]}

货号：A157173 同义名： HS-592 fumarate;Meclastine fumarate

Clemastine fumarate is a selective antagonist of histamine H1 receptor with IC50 of 3 nM.

Clemastine fumarate 化学结构
CAS号：14976-57-9

Clemastine fumarate 3D分子结构
CAS号：14976-57-9

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Clemastine fumarate 纯度/质量文件产品仅供科研

货号：A157173 标准纯度： {[allProObj[0].p_purity_real_show]} 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

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组胺受体亚型比较

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		✔					99%
Betahistine			+ Histamine H3 receptor, IC50: 1.9 μM				98%
Ciproxifan maleate			+++ Histamine H3 receptor, IC50: 9.2 nM				99%+
S 38093			++ human H3 receptor, Ki: 1.2 μM rat H3 receptor, Ki: 1.44 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。

Clemastine fumarate 生物活性

靶点

H1 receptor

Histamine H1 receptor, IC50:3 nM

描述

Clemastine Fumarate is a first-generation histamine receptor H1 (HRH1) antagonist. As a safe and efficient anti-allergic agent, clemastine could impressively alleviate stress-related depressive-like phenotype in mice^[3]. Clemastine fumarate can stimulate differentiation of oligodendrocyte precursor cells in vitro, in animal models, and in human cells^[4]. Clemastine fumarate (CLE) can protect against myocardial ischemia-reperfusion injury (MIRI) through regulation of toll like receptor 4 (TLR4)^[5]. Clemastine, failed to prevent migraine or headache after pituitary adenylate cyclase activating peptide-38 infusion, thus making a role for histamine release or mast cell degranulation in pituitary adenylate cyclase activating peptide-38-induced migraine less likely^[6].

Clemastine fumarate 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
NCT01154361	Angioedema	Phase 2	Completed	-	Germany ... 展开 >> Klinikum rechts der Isar Hals-Nasen-Ohrenklinik der TUM Munich, Bavaria, Germany, 81675 收起 <<
NCT00481676	-		Completed	-	-
NCT01125761	Dermatitis	Phase 3	Withdrawn	-	Brazil ... 展开 >> LAL Clinica Pesquisa e Desenvolvimento Ltda Valinhos, São Paulo, Brazil, 13276-245 LAL Clínica Pesquisa e Desenvolvimento Ltda Valinhos, São Paulo, Brazil, 13276-245 收起 <<

Clemastine fumarate 参考文献

[1]Abbasi MM, Valizadeh H, et al.Inhibitory effect of clemastine on P-glycoprotein expression and function: an in vitro and in situ study. Iran J Basic Med Sci. 2016 Apr;19(4):423-9.

[2]Li Z, He Y, et al. Clemastine rescues behavioral changes and enhances remyelination in the cuprizone mouse model of demyelination. Neurosci Bull. 2015 Oct;31(5):617-25.

[3]Su WJ, Zhang T, Jiang CL, Wang W. Clemastine Alleviates Depressive-Like Behavior Through Reversing the Imbalance of Microglia-Related Pro-inflammatory State in Mouse Hippocampus. Front Cell Neurosci. 2018 Nov 13;12:412

[4]Green AJ, Gelfand JM, Cree BA, Bevan C, Boscardin WJ, Mei F, Inman J, Arnow S, Devereux M, Abounasr A, Nobuta H, Zhu A, Friessen M, Gerona R, von Büdingen HC, Henry RG, Hauser SL, Chan JR. Clemastine fumarate as a remyelinating therapy for multiple sclerosis (ReBUILD): a randomised, controlled, double-blind, crossover trial. Lancet. 2017 Dec 2;390(10111):2481-2489

[5]Yuan X, Juan Z, Zhang R, Sun X, Yan R, Yue F, Huang Y, Yu J, Xia X. Clemastine Fumarate Protects Against Myocardial Ischemia Reperfusion Injury by Activating the TLR4/PI3K/Akt Signaling Pathway. Front Pharmacol. 2020 Feb 10;11:28

[6]Vollesen LH, Guo S, Andersen MR, Ashina M. Effect of the H1-antihistamine clemastine on PACAP38 induced migraine. Cephalalgia. 2019 Apr;39(5):597-607

Clemastine fumarate 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.17mL

0.43mL

0.22mL

10.87mL

2.17mL

1.09mL

21.74mL

4.35mL

2.17mL

Clemastine fumarate 技术信息

CAS号	14976-57-9
分子式	C₂₅H₃₀ClNO₅
分子量	459.96

别名	HS-592 fumarate;Meclastine fumarate;Clemastine (fumarate)
运输	蓝冰

存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Sealed in dry,2-8°C

溶解度

DMSO: 15 mg/mL(32.61 mM)，配合低频超声助溶，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

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

NCT01154361	Angioedema	Phase 2	Completed	-	Germany ... 展开 >> Klinikum rechts der Isar Hals-Nasen-Ohrenklinik der TUM Munich, Bavaria, Germany, 81675 收起 <<
NCT00481676	-		Completed	-	-
NCT01125761	Dermatitis	Phase 3	Withdrawn	-	Brazil ... 展开 >> LAL Clinica Pesquisa e Desenvolvimento Ltda Valinhos, São Paulo, Brazil, 13276-245 LAL Clínica Pesquisa e Desenvolvimento Ltda Valinhos, São Paulo, Brazil, 13276-245 收起 <<
NCT00913549	Allergy	Phase 1	Completed	-	-
NCT02613091	Healthy Subjects	Phase 1	Completed	-	United States, California ... 展开 >> Sandler Neurosciences Building, Neurological Clinical Research Unit San Francisco, California, United States, 94107 收起 <<
NCT00481676	Chronic Urticaria	Phase 2	Completed	-	Germany ... 展开 >> Novartis Investigative Site Berlin, Germany Novartis Investigative Site Bonn, Germany Novartis Investigative Site Dresden, Germany Novartis Investigative Site Giessen, Germany Novartis Investigative Site Hamburg, Germany Novartis Investigative Site Hannover, Germany Novartis Investigative Site Koeln, Germany Novartis Investigative Site Leipzig, Germany Novartis Investigative Site Luebeck, Germany Novartis Investigative Site Mainz, Germany Novartis Investigative Site Munich, Germany 收起 <<
NCT02521311	Optic Neuritis	Phase 2	Recruiting	January 2021	United States, California ... 展开 >> University of California San Francisco Recruiting San Francisco, California, United States, 94158 Contact: Tracy Tran, BA 415-353-2707 tracy.tran@ucsf.edu 收起 <<
NCT02040298	Multiple Sclerosis, Relapsing-... 展开 >>Remitting 收起 <<	Phase 2	Completed	-	United States, California ... 展开 >> UCSF Multiple Sclerosis Center San Francisco, California, United States, 94518 收起 <<
NCT01239719	Allergy Derma... 展开 >>titis 收起 <<	Phase 3	Unknown	December 2011	-
NCT01257061	Eczema	Phase 3	Unknown	August 2013	Brazil ... 展开 >> Medcin instituto da Pele Recruiting Osasco, São Paulo, Brazil, 060323-000 Contact: Flavia Addor 5511 3681 6362 收起 <<

富马酸氯马斯汀 /Clemastine fumarate {[allProObj[0].p_purity_real_show]}

Clemastine fumarate 纯度/质量文件产品仅供科研

全球学术期刊中引用的产品

Clemastine fumarate 质控信息

Clemastine fumarate 生物活性

Clemastine fumarate 临床研究

Clemastine fumarate 参考文献

Clemastine fumarate 实验方案

Clemastine fumarate 技术信息

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富马酸氯马斯汀 /Clemastine fumarate {[allProObj[0].p_purity_real_show]}

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全球学术期刊中引用的产品

Clemastine fumarate 质控信息

Clemastine fumarate 生物活性

Clemastine fumarate 临床研究

Clemastine fumarate 参考文献

Clemastine fumarate 实验方案

Clemastine fumarate 技术信息

最近浏览的产品

大规格询价

摩尔计算器

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总药量计算器

工作液计算器

细胞研究

临床研究

确认信息

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