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Emedastine Difumarate
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Emedastine Difumarate图片
CAS NO:87233-62-3
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品名称
富马酸依美斯汀;富马酸依美司丁
产品介绍
Emedastine difumarate 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,Ki值为 1.3 nM。Emedastine difumarate 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 difumarate is an orally active, selective and high affinityhistamineH1receptorantagonist with aKivalue of 1.3 nM. Emedastine difumarate is a benzimidazole derivative with potent antiallergic properties and used for allergic rhinitis, allergic skin diseases and allergic conjunctivitis[1][2][3].

IC50& Target[1]

H1Receptor

1.3 nM (Ki)

H2Receptor

49067 nM (Ki)

H3Receptor

12430 nM (Ki)

体外研究
(In Vitro)

Emedastine difumarate inhibits histamine H2receptor (Ki=49067 nM) and histamine H3receptor (Ki=12430 nM)[1].
High concentrations of Emedastine difumarate (1 and 10 ng/ml) significantly inhibits type 1 collagen production in normal human dermal fibroblasts[2].
Emedastine difumarate (1, 10, 100, 1000 nM) at concentrations of ≥ 10 nM inhibits CC chemokine-elicited eosinophil migration[2].

体内研究
(In Vivo)

Emedastine difumarate (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[3].
Pretreatment with Emedastine difumarate (0.03, 0.1, 0.3 mg/kg; orally) significantly inhibits the scratching induced by substance P and leukotriene B[3].
Emedastine difumarate (0.3 mg/kg, p.o.) produces significant inhibition of passive peritoneal anaphylaxis in guinea-pigs[2].
Emedastine difumarate inhibits histamine-induced contractions of isolated ileum (IC50=6.1 nM)[2].

Animal Model:Male ICR mice 5-6 weeks of age[3]
Dosage:0.03, 0.1, 0.3 mg/kg
Administration:Orally; 30 min before pruritogen injection
Result:Significantly suppressed histamine-induced scratching with pretreatment of 0.1 and 0.3 mg/kg.
Clinical Trial
分子量

534.56

Formula

C25H34N4O9

CAS 号

87233-62-3

中文名称

富马酸依美斯汀;富马酸依美司丁

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.