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Emedastine/依美斯汀 {[allProObj[0].p_purity_real_show]}

货号:A634117

Emedastine is a potent, high affinity histamine H1-receptor-selective antagonist with Ki of 1.3 ±0.1 nM for H1-receptors while considerably weaker at H2- (Ki = 49,067 ± 11,113 nM) and H3-receptors (Ki = 12,430 ± 1,282 nM).

Emedastine/依美斯汀 化学结构 CAS号:87233-61-2
Emedastine/依美斯汀 化学结构
CAS号:87233-61-2
Emedastine/依美斯汀 3D分子结构
CAS号:87233-61-2
Emedastine/依美斯汀 化学结构 CAS号:87233-61-2
Emedastine/依美斯汀 3D分子结构 CAS号:87233-61-2
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Emedastine/依美斯汀 纯度/质量文件 产品仅供科研

货号:A634117 标准纯度: {[allProObj[0].p_purity_real_show]}
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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。

Emedastine/依美斯汀 生物活性

描述 Emedastine is a high affinity and high potency histamine antagonist with the highest selectivity for the H1-histamine receptor. Emedastine exhibited the highest affinity for H1-receptors (dissociation constant, Ki = 1.3 +/- 0.1 nM), and was considerably weaker at H2- (K1 = 49,067 +/- 11,113 nM) and H3-receptors (Ki = 12,430 +/- 1,282 nM). The H1-selectivity of emedastine was considerably superior to that of pyrilamine (H2:H1, H3:H1 and H2:H3 ratios of 11887, 12709 and 1, respectively). The potency of emedastine (IC50 = 1.44 +/- 0.3 nM) for antagonizing histamine-induced phosphoinositide turnover in human trabecular meshwork cells compared well with its binding affinity at the H1-receptor[1]. Emedastine displays pharmacodynamic properties comparable with cetirizine and therefore qualifies as a safe and alternative compound with H1-receptor antagonist properties[2]. In the Vienna Challenge Chamber model, ketotifen and emedastine both effectively alleviated ocular symptoms of SAC (seasonal allergic conjunctivitis) after single-dose administration[3].

Emedastine/依美斯汀 参考文献

[1]Sharif NA, Su SX, Yanni JM. Emedastine: a potent, high affinity histamine H1-receptor-selective antagonist for ocular use: receptor binding and second messenger studies. J Ocul Pharmacol. 1994 Winter;10(4):653-64

[2]Jansen B, Graselli U, Dallinger S, Kiss B, Wacheck V, Schlagbauer-Wadl H, Assandri A, Müller M. Pharmacokinetics and pharmacodynamics of the novel H1-receptor antagonist emedastine in healthy volunteers. Eur J Clin Pharmacol. 2000 Feb-Mar;55(11-12):837-41

[3]Horak F, Stübner P, Zieglmayer R, Kawina A, Moser M, Lanz R. Onset and duration of action of ketotifen 0.025% and emedastine 0.05% in seasonal allergic conjunctivitis : efficacy after repeated pollen challenges in the vienna challenge chamber. Clin Drug Investig. 2003;23(5):329-37

Emedastine/依美斯汀 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.31mL

0.66mL

0.33mL

16.53mL

3.31mL

1.65mL

33.07mL

6.61mL

3.31mL

Emedastine/依美斯汀 技术信息

CAS号87233-61-2
分子式C17H26N4O
分子量 302.41
SMILES Code CN(CCC1)CCN1C2=NC3=CC=CC=C3N2CCOCC
MDL No. MFCD00865647
别名
运输蓝冰
InChI Key KBUZBQVCBVDWKX-UHFFFAOYSA-N
Pubchem ID 3219
存储条件

In solvent -20°C:3-6个月-80°C:12个月

溶解方案 请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的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
方案一
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