富马酸依美斯汀
| 中文名称 | 富马酸依美斯汀 |
|---|---|
| 中文同义词 | 依美斯汀二富马酸盐;富马酸依美斯汀 USP标准品;富马酸依美斯汀 EP标准品;富马酸依美司汀;1-(2-乙氧基乙基)-2-(六氢-4-甲基-1H-1,4-二氮杂卓-1-基)-1H-苯并咪唑二富马酸盐;富马酸依美达斯汀;1-(2-乙氧基乙基)-2-(4-甲基-1,4-二氮杂环庚-1-基)-1H-苯并[D]咪唑 二富马酸盐;二富马酸依美斯汀 |
| 英文名称 | EMEDASTINE FUMARATE |
| 英文同义词 | 1-(2-ethoxyethyl)-2-(4-methylhexahydro-1h-1,4-diazepin-1-yl)-benzimidazol;1-(2-ethoxyethyl)-2-(4-methylhexahydro-1h-1,4-diazepin-1-yl)benzimidazolefum;1-(2-Ethoxyethyl)-2-(4-methylhexahydro-1H-1,4-diazepine-1-yl)-1H-benzimidazole·bisfumaric acid;Daren;Emedastin difumarate;Emedastin fumarate;Remicut;Emedastine Difumarate (100 mg) |
| CAS号 | 87233-62-3 |
| 分子式 | C25H34N4O9 |
| 分子量 | 534.56 |
| EINECS号 | 805-825-7 |
| 相关类别 | 医药原料药;合成;医药原料药 科研原料;原料药;原料药及中间体;医用原料;化学试剂 |
| Mol文件 | 87233-62-3.mol |
| 结构式 |  |
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 |
| 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
| RTECS号 | DD8870000 |
|---|---|
| 海关编码 | 2933992600 |
| 毒性 | LD50 orally in guinea pigs: 744 mg/kg (Fukuda) |
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/01/16 | S5647 | 富马酸依美斯汀 Emedastine Difumarate | 87233-62-3 | 5mg | 795.16元 |
| 2024/01/16 | S5647 | 富马酸依美斯汀 Emedastine Difumarate | 87233-62-3 | 25mg | 2375.53元 |