富马酸依美斯汀
富马酸依美斯汀 性质
| 熔点 | 148-151° |
|---|---|
| 储存条件 | 2-8°C |
| 溶解度 | 易溶于水，微溶于无水乙醇，极微溶于丙酮。 |
| Merck | 14,3557 |
| 主要应用 | 药物（小分子） |
| InChIKey | FWLKKPKZQYVAFR-LVEZLNDCSA-N |
| SMILES | C1(=NC2C=CC=CC=2N1CCOCC)N1CCN(C)CCC1.C(/C(=O)O)=C\C(=O)O.C(/C(=O)O)=C\C(=O)O |
富马酸依美斯汀 用途与合成方法
| Target | Value |
|
Histamine H1 receptor
() |
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.
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. |
安全信息
| WGK Germany | WGK 3 |
|---|---|
| RTECS号 | DD8870000 |
| 海关编码 | 2933992600 |
| 存储类别 | 11 - 可燃固体 |
| 危险性类别 | 急性毒性 类别4 经口 |
| 毒性 | LD50 orally in guinea pigs: 744 mg/kg (Fukuda) |
富马酸依美斯汀 价格(试剂级)
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2026-07-06 | S5647 | 富马酸依美斯汀 | 87233-62-3 | 5mg | 795.16 |
| 2026-07-06 | S5647 | 富马酸依美斯汀 | 87233-62-3 | 25mg | 2375.53 |
