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CAS No.: 182349-12-8

Rupatadine Fumarate/富马酸卢帕他定 Catalog No. CSN12316

Synonyms: UR-12592 Fumarate;Rupatadine (fumarate);Rupafin

Rupatadine fumarate is an inhibitor of PAFR and histamine (H1) receptor with Ki of 550 nM and 102 nM, respectively.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 Histamine Receptor H1

Ki:102nM PAFR

Ki:550nM
描述Rupatadine fumarate is a second-generation antihistamine provided with a potent, long-lasting and balanced in vivo dual platelet-activating factor (PAF) and histamine antagonist activity and it uniquely combines both activities at a high level of potency. Rupatadine has a rapid onset of action and a long-lasting effect, so a once-daily dosing is permitted, moreover is well tolerated by young adults and the elders^[3]. Rupatadine is indicated for the treatment of allergic rhinitis and urticaria^[4]. New studies have demonstrated that rupatadine inhibits PAF effects in nasal airways and produces a greater reduction in nasal symptoms than levocetirizine^[5]. Rupatadine 20 and 40 mg significantly reduced the development of chronic cold urticaria symptom without an increase in adverse effects^[6]. Moreover, rupatadine significantly reduced endothelial permeability by dengue sera in vitro, and significantly inhibited the increased haematocrit in dengue-infected mice with dose-dependency^[7].
参考文献

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.8796 mL
- 9.3980 mL
- 18.7959 mL
- 5 mM
- 0.3759 mL
- 1.8796 mL
- 3.7592 mL
- 10 mM
- 0.1880 mL
- 0.9398 mL
- 1.8796 mL

技术信息

CAS号

182349-12-8

储存条件

粉末: Sealed in dry,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C30H30ClN3O4

运输

蓝冰

分子量

532.03

别名

UR-12592 Fumarate;Rupatadine (fumarate);Rupafin;Alergoliber;Rinialer;Pafinur;Rupax;Ralif;富马酸卢帕他定

溶解度

DMSO	9.0 mg/mL (16.9 mM)
Water	Insoluble
Ethanol	12.0 mg/mL (22.6 mM)

动物实验配方

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靶点	Description	IC50
Histamine Receptor H1		Ki:102nM
PAFR		Ki:550nM

Rupatadine Fumarate/富马酸卢帕他定 Catalog No. CSN12316

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