中文名称: | 富马酸依美斯汀 | ||||
---|---|---|---|---|---|
英文名称: | Emedastine difumarate | ||||
别名: | 富马酸依美司丁;1-(2-乙氧基乙基)-2-(4-甲基-1-哌嗪基)苯并咪唑富马酸盐 1-(2-Ethoxyethyl)-2-(4-methyl-1-homopiperazinyl)benzimidazole Difumarate | ||||
CAS No: | 87233-62-3 | 分子式: | C25H34N4O9 | 分子量: | 534.56 |
CAS No: | 87233-62-3 | ||||
分子式: | C25H34N4O9 | ||||
分子量: | 534.56 |
基本信息
产品编号: |
E70086 |
||||
产品名称: |
Emedastine difumarate |
||||
CAS: |
87233-62-3 |
储存条件 |
粉末 |
-20℃ |
四年 |
分子式: |
溶于液体 |
-80℃ |
6个月 |
||
分子量: |
534.56 |
|
|
||
化学名: |
1-(2-Ethoxyethyl)-2-(4-methyl-1-homopiperazinyl)benzimidazole Difumarate |
||||
Solubility (25°C): |
|||||
体外:
|
DMSO |
100mg/mL (187.06mM) |
|||
Ethanol |
21mg/mL (39.28mM) |
||||
Water |
100mg/mL (187.06mM) |
||||
体内(现配现用): |
|
||||
<1mg/ml表示微溶或不溶。 |
|||||
普西唐提供的所有化合物浓度为内部测试所得,实际溶液度可能与公布值有所偏差,属于正常的批间细微差异现象。 |
|||||
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;⼀旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 |
制备储备液
浓度
溶液体积 质量 |
1mg |
5mg |
10mg |
1mM |
1.8707mL |
9.3535mL |
18.7070mL |
5mM |
0.3741mL |
1.8707mL |
3.7414mL |
10mM |
0.1871mL |
0.9353mL |
1.8707mL |
50mM |
0.0374mL |
0.1871mL |
0.3741mL |
生物活性
产品描述 |
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 1.3nM。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 |
H1 Receptor 1.3nM (Ki) |
H2 Receptor 49067nM (Ki) |
H3 Receptor 12430nM (Ki) |
|
体外研究 |
Emedastine difumarate inhibits histamine H2 receptor (Ki=49067nM) and histamine H3 receptor (Ki=12430nM).High concentrations of Emedastine difumarate (1 and 10ng/ml) significantly inhibits type 1 collagen production in normal human dermal fibroblasts.Emedastine difumarate (1,10,100,1000nM) at concentrations of≥10nM inhibits CC chemokine-elicited eosinophil migration. |
|||
体内研究 |
Emedastine difumarate (0.03,0.1,0.3mg/kg;orally;pretreatment of 30 min) significantly suppresses histamine-induced scratching with 0.1 and 0.3mg/kg but not 0.03mg/kg.Pretreatment with Emedastine difumarate (0.03,0.1,0.3mg/kg;orally) significantly inhibits the scratching induced by substance P and leukotriene B.Emedastine difumarate (0.3mg/kg,p.o.) produces significant inhibition of passive peritoneal anaphylaxis in guinea-pigs.Emedastine difumarate inhibits histamine-induced contractions of isolated ileum (IC50=6.1nM). |
|||
Animal Model: |
Male ICR mice 5-6 weeks of age |
|||
Dosage: |
0.03,0.1,0.3mg/kg |
|||
Administration: |
Orally;30 min before pruritogen injection |
|||
Result: |
Significantly suppressed histamine-induced scratching with pretreatment of 0.1 and 0.3mg/kg. |
本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)
摩尔浓度计算公式
用本工具协助配置特定浓度的溶液,使用的计算公式为:
开始浓度 x 开始体积 = 最终浓度 x 最终体积
稀释公式
稀释公式一般简略地表示为:C1V1 = C2V2 ( 输入 输出 )