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Rupatadine Fumarate

产品编号 T6242 CAS 182349-12-8

别名: 富马酸卢帕他定, Rinialer, Rupafin, Alergoliber

Rupatadine Fumarate (Rinialer) 是一种可口服的长效PAF/H1受体的双抑制剂，Ki 值分别为 0.55 μM 和 0.1 μM。它可研究过敏性鼻炎和荨麻疹。

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Rupatadine Fumarate, CAS 182349-12-8

规格	价格/CNY	货期
50 mg	￥ 451	现货
100 mg	￥ 632	现货
500 mg	￥ 1,234	现货
1 mL * 10 mM (in DMSO)	￥ 179	现货

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其他形式的 Rupatadine Fumarate:

Rupatadine
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纯度: 99.64%

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生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

产品描述	Rupatadine Fumarate (Rinialer) (UR-12592 Fumarate) is a potent dual PAF/H1 antagonist with Ki of 0.55/0.1 uM.
靶点活性	PAFR:550 nM(Ki), H1 receptor:102 nM(Ki)
体外活性	Rupatadine inhibits both platelet-activating factor (PAF) and histamine (H1) effects through its interaction with specific receptors. Rupatadine competitively inhibits histamine-induced guinea pig ileum contraction (pA2 = 9.29 ± 0.06) without affecting contraction induced by ACh, serotonin or leukotriene D4(LTD4). It also competitively inhibits PAF-induced platelet aggregation in washed rabbit platelets (WRP) (pA2= 6.68 ± 0.08) and in human platelet-rich plasma (HPRP) (IC50 = 0.68 μM), while not affecting ADP- or arachidonic acid-induced platelet aggregation. [1] In another study, it is reported rupatadine and loratadine shows similar inhibitory effect on histamine and TNF-α release, whereas SR-27417A only exhibits inhibitory effect against TNF-α. [2]
体内活性	Rupatadine blocks histamine- and PAF-induced effects in vivo, such as hypotension in rats (ID50 = 1.4 and 0.44 mg/kg i.v., respectively) and bronchoconstriction in guinea pigs (ID50 = 113 and 9.6 μg/kg i.v.). Moreover, it potently inhibits PAF-induced mortality in mice (ID50 = 0.31 and 3.0 mg/kg i.v. and p.o., respectively) and endotoxin-induced mortality in mice and rats (ID50 = 1.6 and 0.66 mg/kg i.v.). Rupatadine's duration of action is long, as assessed by the histamine- and PAF-induced increase in vascular permeability test in dogs (42 and 34% inhibition at 26 h after 1 mg/kg p.o.). Rupatadine at a dose of 100 mg/kg p.o. neither modifies spontaneous motor activity nor prolongs barbiturate-sleeping time in mice, which indicates a lack of sedative effects. [1]
激酶实验	[3H]-Pyrilamine binding to histamine (H1) receptors in guinea pig cerebellum membranes.: Antagonists are incubated with guinea pig cerebellum membranes (0.6 mg/ml) and [3H]-pyrilamine (1.2 nM) in 0.5 ml 50 mM PBS, pH 7.5, for 30 min at 25 ℃. The incubation is ended by the addition of 5 ml of ice-cold PBS containing 2 μM pyrilamine and the collection of membranes on Whatman GF/B filters. Then the filters are washed with 3 × 5 ml of ice-cold PBS plus 2 μM pyrilamine and transferred to counting vials. The radioactivity retained by each filter is measured by liquid scintillation counting in 3 ml of HiSafe 3. Specific binding is determined from the difference between the [3H]-pyrilamine bound in the absence and in the presence of a large molar excess (10 μM) of unlabeled promethazine.
细胞实验	Platelet aggregation is induced by C18-PAF and measured by using a dual-channel aggregometer Chrono-log 560. Platelet aggregation in the absence and in the presence (5-min incubation) of the test compounds is recorded. Activity of the inhibitors is expressed as the IC50 values. To assess selectivity, rupatadine is tested against other aggregating agents, including arachidonic acid (1 mM) and ADP (5 μM), in WRP. Dose-response curves for PAF-induced aggregation in WRP are obtained in the absence of rupatadine and in its presence at various concentrations (3 × 10-7–3 × 10-5 M).(Only for Reference)

别名	富马酸卢帕他定, Rinialer, Rupafin, Alergoliber
分子量	532.03
分子式	C26H26ClN3·C4H4O4
CAS No.	182349-12-8

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

Ethanol: 11 mg/mL (20.7 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 9 mg/mL (16.91 mM)

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
Ethanol / DMSO	1 mM	1.8796 mL	9.398 mL	18.7959 mL	46.9898 mL
	5 mM	0.3759 mL	1.8796 mL	3.7592 mL	9.398 mL
	10 mM	0.188 mL	0.9398 mL	1.8796 mL	4.699 mL
Ethanol	20 mM	0.094 mL	0.4699 mL	0.9398 mL	2.3495 mL

计算器

摩尔浓度计算器

稀释计算器

配液计算器

分子量计算器

质量

浓度

容积

分子量

浓度 (起始)

容积 (起始)

浓度 (终)

容积 (终)

溶液体积

质量

配液浓度

参考文献

1. Merlos M, et al. J Pharmacol Exp Ther, 1997, 280(1), 114-121. 2. Queralt M, et al. Inflamm Res, 2000, 49(7), 355-360. 3. Barbanoj MJ, et al. Neuropsychobiology, 2004, 50(4), 311-321. 4. Sudhakara Rao M, et al. Indian J Otolaryngol Head Neck Surg, 2009, 61(4), 320-332.

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

剂量

mg/kg

每只动物体重

给药体积

μL

动物数量

第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到，包括如何准备库存溶液，如何存储产品，以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

Rupatadine Fumarate 182349-12-8 Autophagy GPCR/G Protein Immunology/Inflammation Neuroscience PAFR Histamine Receptor urticaria PAF UR12592 Inhibitor inhibit allergic UR-12592 富马酸卢帕他定 Rinialer Rupafin Rupatadine rhinitis Alergoliber UR 12592 inhibitor

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Rupatadine Fumarate

存储

溶解度

溶液配制表

计算器

输入分子式，点击计算，可计算出产品的分子量。

参考文献

相关产品

相关化合物库

剂量换算

体内实验配液计算器

技术支持

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