Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
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 |
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 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ethanol: 11 mg/mL (20.7 mM)
H2O: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 9 mg/mL (16.91 mM)
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 |
对于不同动物的给药剂量换算,您也可以参考 更多...
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。
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。
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