富马酸依美斯汀
- CAS号:87233-62-3
- 英文名:EMEDASTINE FUMARATE
- 中文名:富马酸依美斯汀
- CBNumber:CB6714475
- 分子式:C25H34N4O9
- 分子量:534.56
- MOL File:87233-62-3.mol
- 熔点 :148-151°
- 储存条件 :2-8°C
- 溶解度 :Soluble in water, sparingly soluble in anhydrous ethanol, very slightly soluble in acetone.
- Merck :14,3557
- RTECS号 :DD8870000
- 海关编码 :2933992600
- 毒性 :LD50 orally in guinea pigs: 744 mg/kg (Fukuda)
富马酸依美斯汀性质、用途与生产工艺
- 生物活性 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。
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靶点
Target Value Histamine H1 receptor
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体外研究
Emedastine difumarate inhibits histamine H 2 receptor (K i =49067 nM) and histamine H 3 receptor (K i =12430 nM).
High concentrations of Emedastine difumarate (1 and 10 ng/ml) significantly inhibits type 1 collagen production in normal human dermal fibroblasts.
Emedastine difumarate (1, 10, 100, 1000 nM) at concentrations of ≥ 10 nM inhibits CC chemokine-elicited eosinophil migration. -
体内研究
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.
Pretreatment with Emedastine difumarate (0.03, 0.1, 0.3 mg/kg; orally) significantly inhibits the scratching induced by substance P and leukotriene B.
Emedastine difumarate (0.3 mg/kg, p.o.) produces significant inhibition of passive peritoneal anaphylaxis in guinea-pigs.
Emedastine difumarate inhibits histamine-induced contractions of isolated ileum (IC 50 =6.1 nM).
Animal Model: Male ICR mice 5-6 weeks of age 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.
- 更新日期：2024/11/08
- 产品编号：S5647
- 产品名称：富马酸依美斯汀 Emedastine Difumarate
- CAS编号：87233-62-3
- 包装：5mg
- 价格：795.16元
- 更新日期：2024/11/08
- 产品编号：S5647
- 产品名称：富马酸依美斯汀 Emedastine Difumarate
- CAS编号：87233-62-3
- 包装：25mg
- 价格：2375.53元
- 公司名称：EDQM
- 联系电话：--
- 电子邮件：orders@edqm.eu
- 国家：法国
- 产品数：1913
- 优势度：81
