依美司丁
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- CAS号:
- 87233-61-2
- 英文名:
- Emedastine
- 英文别名:
- EMEDASTINE;Emedastine impurity F;Emedastine Impurity 14;1-(2-Ethoxyethyl)-2-(4-methyl-1,4-diazepan-1-yl)benzimidazole;1-(2-Ethoxyethyl)-2-(4-methyl-1,4-diazepan-1-yl)-1H-benzimidazole;1-(2-ethoxyethyl)-2-(4-Methyl-1,4-diazepan-1-yl)-1H-1,3-benzodiazole;1-(2-ethoxyethyl)-2-(4-methyl-1,4-diazepan-1-yl)-1H-benzo[d]imidazole;1-(2-Ethoxyethyl)-2-(4-methylhexahydro-1H-1,4-diazepine-1-yl)-1H-benzimidazole;1-(2-Ethoxyethyl)-2-[(hexahydro-4-methyl-1H-1,4-diazepin)-1-yl]-1H-benzimidazole;allergic,Histamine Receptor,antiallergic,benzimidazole,Inhibitor,skin,inhibit,Emedastine,orally,rhinitis,diseases,conjunctivitis
- 中文名:
- 依美司丁
- 中文别名:
- 依美斯汀;依美司丁;依美斯汀杂质F;依美斯汀杂质E;依美斯汀杂质D;依美斯汀杂质C;依美斯汀杂质B;依美斯汀杂质14;1-(2-乙氧基乙基)-2-(4-甲基-1,4-二氮杂庚烷-1-基)苯并咪唑;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
- CBNumber:
- CB8728076
- 分子式:
- C17H26N4O
- 分子量:
- 302.41
- MOL File:
- 87233-61-2.mol
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依美司丁化学性质
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沸点:
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446.6±55.0 °C(Predicted)
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密度:
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1.15±0.1 g/cm3(Predicted)
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储存条件:
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2-8°C
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溶解度:
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DMSO: 125 mg/mL (413.35 mM); Ethanol: 100 mg/mL (330.68 mM)
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酸度系数(pKa):
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8.86±0.10(Predicted)
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CAS 数据库:
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87233-61-2(CAS DataBase Reference)
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依美司丁性质、用途与生产工艺
依美斯汀（Emedastine，商品名称： Emadine）是第二代抗组织胺，可用作眼药水以减缓过敏性结膜炎的症状。依美斯汀属于H1 接收器抑制剂。借由抑制组织胺的作用来减缓过敏性结膜炎的症状。当依美斯汀用作眼药水时，会以双延胡索酸盐（difumarate）的形式存在。
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，Ki 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。
| Target | Value |
H1 receptor
(Cell-free assay)
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1.3 nM(Ki)
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Emedastine inhibits histamine H
2
receptor (K
i
=49067 nM) and histamine H
3
receptor (K
i
=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.
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).
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Animal Model:
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Male ICR mice 5-6 weeks of age
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Dosage:
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0.03, 0.1, 0.3 mg/kg
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Administration:
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Orally; 30 min before pruritogen injection
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Result:
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Significantly suppressed histamine-induced scratching with pretreatment of 0.1 and 0.3 mg/kg.
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依美司丁
上下游产品信息
上游原料
下游产品
| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
|---|
| 2024/01/25 | HY-108411 | Emedastine | | 1 mg | 288元 |
| 2024/01/25 | HY-108411 | 依美司丁
Emedastine | 87233-61-2 | 5mg | 720元 |
依美司丁
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87233-61-2, 依美司丁 相关搜索:
- DCP
- impurity
- 合成有机化合物配体
- 化学试剂
- 原料药
- 杂质对照品
- 杂质世界-依美斯汀
- C17H26N4O
- 依美斯汀杂质14
- 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
- 依美斯汀杂质F
- 依美斯汀杂质E
- 依美斯汀杂质D
- 依美斯汀杂质C
- 依美斯汀杂质B
- 1-(2-乙氧基乙基)-2-(4-甲基-1,4-二氮杂庚烷-1-基)苯并咪唑
- 依美斯汀
- 依美司丁
- 87233-61-2
- Emedastine Impurity 14
- allergic,Histamine Receptor,antiallergic,benzimidazole,Inhibitor,skin,inhibit,Emedastine,orally,rhinitis,diseases,conjunctivitis
- Emedastine impurity F
- 1-(2-ethoxyethyl)-2-(4-methyl-1,4-diazepan-1-yl)-1H-benzo[d]imidazole
- 1-(2-Ethoxyethyl)-2-(4-methyl-1,4-diazepan-1-yl)-1H-benzimidazole
- 1-(2-ethoxyethyl)-2-(4-Methyl-1,4-diazepan-1-yl)-1H-1,3-benzodiazole
- 1-(2-Ethoxyethyl)-2-[(hexahydro-4-methyl-1H-1,4-diazepin)-1-yl]-1H-benzimidazole
- 1-(2-Ethoxyethyl)-2-(4-methylhexahydro-1H-1,4-diazepine-1-yl)-1H-benzimidazole
- 1-(2-Ethoxyethyl)-2-(4-methyl-1,4-diazepan-1-yl)benzimidazole
- EMEDASTINE