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87233-62-3

中文名称 富马酸依美斯汀
英文名称 EMEDASTINE FUMARATE
CAS 87233-62-3
分子式 C25H34N4O9
分子量 534.56
MOL 文件 87233-62-3.mol
更新日期 2024/04/24 11:40:36
87233-62-3 结构式 87233-62-3 结构式

基本信息

中文别名
富马酸依美司汀
富马酸依美达斯汀
依美斯汀二富马酸盐
富马酸依美斯汀 EP标准品
富马酸依美斯汀 USP标准品
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
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
英文别名
Daren
kb2413
Remicut
Emadine
kb-2413
kg-2413
Rapimine
AL 3432A
ly188695
arate(1:2)
所属类别
原料药

物理化学性质

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.
形态neat
Merck14,3557

安全数据

危险性符号(GHS)
GHS07
警示词警告
危险性描述H302
RTECS号DD8870000
海关编码2933992600
毒性LD50 orally in guinea pigs: 744 mg/kg (Fukuda)
富马酸依美斯汀价格(试剂级)
报价日期产品编号产品名称CAS号包装价格
2024/01/16S5647富马酸依美斯汀
Emedastine Difumarate
87233-62-35mg795.16元
2024/01/16S5647富马酸依美斯汀
Emedastine Difumarate
87233-62-325mg2375.53元
2022/07/01E0936富马酸依美斯汀
Emedastine Difumarate
87233-62-31g2655元

常见问题列表

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。
靶点
TargetValue
Histamine H1 receptor
()
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.
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