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依巴斯汀 /Ebastine {[allProObj[0].p_purity_real_show]}

货号:A124731 同义名: LAS-W 090;RP64305

Ebastine is a selective H1-histamine receptor antagonist.

Ebastine 化学结构 CAS号:90729-43-4
Ebastine 化学结构
CAS号:90729-43-4
Ebastine 3D分子结构
CAS号:90729-43-4
Ebastine 化学结构 CAS号:90729-43-4
Ebastine 3D分子结构 CAS号:90729-43-4
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Ebastine 纯度/质量文件 产品仅供科研

货号:A124731 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 ++

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。

Ebastine 生物活性

靶点
  • H1 receptor

描述 Ebastine is a second-generation histamine H1 receptor antagonist that is used to attenuate allergic inflammation. Ebastine was shown to significantly increase the proliferation of HFDPC (human follicle dermal papilla cells)[3]. Ebastine is a well-established second generation oral H1-antihistamine that is administered once daily at a dose of 10 - 20 mg and is available both as a standard tablet and as a fast-dissolving tablet that disintegrates in the mouth. Ebastine has been shown to relieve symptoms in patients with allergic rhinitis or urticaria in multiple clinical trials. Ebastine is generally well tolerated at recommended doses[4]. Pooled data from clinical efficacy trials of ebastine 1 - 30 mg/day administered for 2 - 3 weeks showed no clinically relevant cardiac effects as assessed by serial electrocardiographs and Holter monitoring[5]. Ebastine 10 mg daily is a well tolerated and effective treatment for allergic rhinitis and chronic idiopathic urticaria[6]. Ebastine 20 mg/day is indicated in patients with moderate and severe allergic symptoms, it has no relevant effects on the psychomotor performance[7].

Ebastine 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
NCT01144832 Irritable Bowel Syndrome Phase 4 Completed - Belgium ... 展开 >> University hospitals Leuven Leuven, Vlaams-Brabant, Belgium, 3000 收起 <<
NCT01940393 Urticaria Phase 4 Completed - Colombia ... 展开 >> Medellin Medellin, Antioquia, Colombia 收起 <<
NCT02065440 Cough Not Applicable Unknown - Korea, Republic of ... 展开 >> Division of Pulmonary and Critical Care Medicine, Department of Internal Medicine, Seoul Metropolitan Government, Seoul National University Boramae Medical Center Seoul, Dongjak-Gu, Korea, Republic of, 156-707 收起 <<

Ebastine 参考文献

[1]Rapolu R, Pandey AK, et al. A novel UV degradation product of Ebastine: isolation and characterization using Q-TOF, NMR, IR and computational chemistry. J Pharm Biomed Anal. 2015 Mar 25;107:488-94.

[2]Ko CM, Ducic I, et al. Suppression of mammalian K+ channel family by ebastine. J Pharmacol Exp Ther. 1997 Apr;281(1):233-44.

[3]Tsai FM, Li CH, Wang LK, Chen ML, Lee MC, Lin YY, Wang CH. Extracellular Signal-Regulated Kinase Mediates Ebastine-Induced Human Follicle Dermal Papilla Cell Proliferation. Biomed Res Int. 2019 Feb 11;2019:6360503

[4]Sastre J. Ebastine in the Treatment of Allergic Rhinitis and Urticaria: 30 Years of Clinical Studies and Real-World Experience. J Investig Allergol Clin Immunol. 2020;30(3):156-168

[5]Moss AJ, Chaikin P, Garcia JD, Gillen M, Roberts DJ, Morganroth J. A review of the cardiac systemic side-effects of antihistamines: ebastine. Clin Exp Allergy. 1999 Jul;29 Suppl 3:200-5

[6]Hurst M, Spencer CM. Ebastine: an update of its use in allergic disorders. Drugs. 2000 Apr;59(4):981-1006

[7]Van Cauwenberge P, De Belder T, Sys L. A review of the second-generation antihistamine ebastine for the treatment of allergic disorders. Expert Opin Pharmacother. 2004 Aug;5(8):1807-13

Ebastine 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.13mL

0.43mL

0.21mL

10.65mL

2.13mL

1.06mL

21.29mL

4.26mL

2.13mL

Ebastine 技术信息

CAS号90729-43-4
分子式C32H39NO2
分子量 469.658
别名 LAS-W 090;RP64305;Kestin;Evastel;Busidril;Bactil;Ebatrol;Aleva;Ebastel;Kestine;Brand name: Evastin
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Keep in dark place,Sealed in dry,Room Temperature

溶解度

DMSO: 7 mg/mL(14.9 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

无水乙醇: 55 mg/mL(117.11 mM),配合低频超声助溶,注意:无水乙醇开封后,易挥发,也会吸收空气中的水分,导致溶解能力下降,请避免使用开封较久的乙醇

动物实验配方

IP 2% DMSO+2% Tween80+30% PEG300+water 6 mg/mL clear

PO 0.5% CMC-Na 38 mg/mL suspension

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