Emedastine|87233-61-2|(依美斯汀)-陌孚医药/Medlife

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Emedastine (Synonyms: 依美斯汀)

目录号: PL14973 纯度: ≥98.0%

CAS No. :87233-61-2

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中文名称	Emedastine
中文别名	依美司丁;依美斯汀;1-(2-乙氧基乙基)-2-(4-甲基-1,4-二氮杂庚烷-1-基)苯并咪唑
英文名称	Emedastine
英文别名	Emedastine;1-(2-ethoxyethyl)-2-(4-methyl-1,4-diazepan-1-yl)benzimidazole;1-(2-ethoxyethyl)-2-(4-methyl-1,4-diazepan-1-yl)-1H-benzo[d]imidazole;1-[2-(ethoxy)ethyl]-2-(4-methyl-1-homopiperazinyl)benzimidazole;1-methyl-4-(1-(2-ethoxyethyl)-1H-benzimidazol-2-yl)[1,4]diazepane;Emadine;Emedastina;Emedastina [INN-Spanish];Emedastine [INN];Emedastinum;Emedastinum [INN-Latin];UNII-9J1H7Y9OJV
Cas No.	87233-61-2
分子式	C₁₇H₂₆N₄O
分子量	302.41
包装储存	Pure form -20°C 3 years；4°C 2 years

产品详情

Emedastine 是一种具有口服活性，选择性和高亲和力的组胺 H₁ 受体拮抗剂，K_i 值为 1.3 nM。Emedastine 是一种苯并咪唑衍生物，具有强大的抗过敏特性，可用于过敏性鼻炎，过敏性皮肤疾病和过敏性结膜炎。

生物活性

Emedastine is an orally active, selective and high affinity histamine H 1 receptor antagonist with a K i value of 1.3 nM. Emedastine is a benzimidazole derivative with potent antiallergic properties and used for allergic rhinitis, allergic skin diseases and allergic conjunctivitis.

性状

Oil

IC50 & Target[1][2]

H1 Receptor 1.3 nM (Ki) H2 Receptor <

体外研究(In Vitro)

Emedastine inhibits histamine H2 receptor (Ki=49067 nM) and histamine H3 receptor (Ki=12430 nM).
High concentrations of Emedastine (1 and 10 ng/ml) significantly inhibits type 1 collagen production in normal human dermal fibroblasts.
Emedastine (1, 10, 100, 1000 nM) at concentrations of ≥ 10 nM inhibits CC chemokine-elicited eosinophil migration. has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

Emedastine (0.03, 0.1, 0.3 mg/kg; orally; pretreatment of 30 min) significantly suppresses histamine-induced scratching with 0.1 and 0.3 mg/kg but not 0.03 mg/kg.
Pretreatment with Emedastine (0.03, 0.1, 0.3 mg/kg; orally) significantly inhibits the scratching induced by substance P and leukotriene B.
Emedastine (0.3 mg/kg, p.o.) produces significant inhibition of passive peritoneal anaphylaxis in guinea-pigs.
Emedastine inhibits histamine-induced contractions of isolated ileum (IC 50 =6.1 nM).
has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Pure form -20°C 3 years；4°C 2 years

ClinicalTrial

参考文献

[1]. Sharif NA, et al. 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]. Murota H, et al. Emedastine difumarate: a review of its potential ameliorating effect for tissue remodeling in allergic diseases. Expert Opin Pharmacother. 2009 Aug;10(11):1859-67.

溶解度数据	In Vitro: DMSO : 125 mg/mL (413.35 mM; Need ultrasonic)Ethanol : 100 mg/mL (330.68 mM; Need ultrasonic)配制储备液

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Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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