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/ 组胺受体 / Rupatadine Fumarate

富马酸卢帕他定 /Rupatadine Fumarate {[allProObj[0].p_purity_real_show]}

货号：A160823 同义名： UR-12592 Fumarate;Rupatadine (fumarate)

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

Rupatadine Fumarate 化学结构 CAS号：182349-12-8
Rupatadine Fumarate 化学结构
CAS号：182349-12-8
Rupatadine Fumarate 3D分子结构
CAS号：182349-12-8
Rupatadine Fumarate 化学结构 CAS号：182349-12-8
Rupatadine Fumarate 3D分子结构 CAS号：182349-12-8
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Rupatadine Fumarate 纯度/质量文件 产品仅供科研

货号：A160823 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

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产品名称 H1 receptor ↓ H2 receptor ↓ H3 receptor ↓ H4 receptor ↓ Histamine receptor ↓ 其他靶点 纯度
Hydroxyzine 2HCl 99+%
Cyclizine ✔ 97%
Loratadine +

B(0)AT2, IC50: 4 μM

 		98%
Desloratadine ++

Histamine H1 receptor, IC50: 51 nM

 		98%
Doxylamine succinate ✔ 99%
Ebastine ✔ 98%
Tripelennamine HCl +

H1 receptor, IC50: 30 μM

 		98%
Meclizine dihydrochloride ✔ 98%
Chlorpheniramine maleate +++

Histamine H1 receptor, IC50: 12 nM

 		99%
Diphenhydramine HCl ✔ 99%
Alcaftadine ++++

H1 receptor, pKi: 8.5

 		++

H2 receptor, pKi: 7.2

 		99%+
Fexofenadine HCl ++

Histamine H1 receptor, IC50: 246 nM

 		99%+
Bilastine +++

H1 receptor, Ki: 44.15 nM

 		98%
Pemirolast potassium ✔ 98%
Bepotastine besilate +

Histamine H1 receptor, pIC50: 5.7

 		98%
Mizolastine +++

Histamine H1 receptor, IC50: 47 nM

 		98%
Brompheniramine maleate ✔ 98%
Carbinoxamine maleate salt ✔ 99+%
Clemastine fumarate ++++

Histamine H1 receptor, IC50: 3 nM

 		98%
Ketotifen fumarate salt ✔ 95%
Rupatadine Fumarate ++

Histamine H1 receptor, Ki: 102 nM

 		PAFR 98%
Famotidine ✔ 97%
Roxatidine Acetate HCl +

Histamine H2 receptor, IC50: 3.2 μM

 		98%
Lafutidine ✔ 99%
Cimetidine ✔ 98%
Nizatidine ++++

Histamine H2 receptor, IC50: 0.9 nM

 		AChE 98%
Ranitidine ✔ 98%
Betahistine +

Histamine H3 receptor, IC50: 1.9 μM

 		98%
Ciproxifan maleate +++

Histamine H3 receptor, IC50: 9.2 nM

 		99%+
S 38093 ++

human H3 receptor, Ki: 1.2 μM

rat H3 receptor, Ki: 1.44 μM

 		98%
JNJ-7777120 ++++

Histamine H4 receptor, Ki: 4.5 nM

 		98%
Azelastine HCl ✔ 98%
Epinastine HCl ✔ 98%
Levodropropizine ✔ 97%
Cyproheptadine hydrochloride ✔ 98%
Hesperetin ✔ 97%
Olopatadine HCl ✔ 98%
Mianserin hydrochloride ✔ 99+%
Buclizine 2HCl ✔ 97%
Latrepirdine 2HCl ✔ GluR 98%
Cetirizine 2HCl ✔ 98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Rupatadine Fumarate 生物活性

靶点

  • H1 receptor

    Histamine H1 receptor, Ki:102 nM
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].

Rupatadine Fumarate 参考文献

[1]Queralt M, Brazis P, et al. In vitro inhibitory effect of rupatadine on histamine and TNF-alpha release from dispersed canine skin mast cells and the human mast cell line HMC-1. Inflamm Res. 2000 Jul;49(7):355-60.

[2]Merlos M, Giral M, et al. Rupatadine, a new potent, orally active dual antagonist of histamine and platelet-activating factor (PAF). J Pharmacol Exp Ther. 1997 Jan;280(1):114-21.

[3]Nettis E, Delle Donne P, Di Leo E, Calogiuri GF, Ferrannini A, Vacca A. Rupatadine for the treatment of urticaria. Expert Opin Pharmacother. 2013 Sep;14(13):1807-13

[4]González-Núñez V, Bachert C, Mullol J. Rupatadine: global safety evaluation in allergic rhinitis and urticaria. Expert Opin Drug Saf. 2016 Oct;15(10):1439-48

[5]Mullol J, Bousquet J, Bachert C, Canonica GW, Giménez-Arnau A, Kowalski ML, Simons FE, Maurer M, Ryan D, Scadding G. Update on rupatadine in the management of allergic disorders. Allergy. 2015 Jan;70 Suppl 100:1-24

[6]Abajian M, Curto-Barredo L, Krause K, Santamaria E, Izquierdo I, Church MK, Maurer M, Giménez-Arnau A. Rupatadine 20 mg and 40 mg are Effective in Reducing the Symptoms of Chronic Cold Urticaria. Acta Derm Venereol. 2016 Jan;96(1):56-9

[7]Malavige GN, Wijewickrama A, Fernando S, Jeewandara C, Ginneliya A, Samarasekara S, Madushanka P, Punchihewa C, Paranavitane S, Idampitiya D, Wanigatunga C, Dissanayake H, Prathapan S, Gomes L, Aman SAB, John AS, Ogg GS. A preliminary study on efficacy of rupatadine for the treatment of acute dengue infection. Sci Rep. 2018 Mar 1;8(1):3857

Rupatadine Fumarate 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.88mL

0.38mL

0.19mL

9.40mL

1.88mL

0.94mL

18.80mL

3.76mL

1.88mL

Rupatadine Fumarate 技术信息

CAS号182349-12-8
分子式C30H30ClN3O4
分子量 532.03
别名 UR-12592 Fumarate;Rupatadine (fumarate)
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Sealed in dry,Room Temperature
溶解度

DMSO: 30 mg/mL(56.39 mM)，配合低频超声，并水浴加热至45℃助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方

Tags: Rupatadine | 182349-12-8 | UR-12592 | UR12592 | UR 12592 | Dual PAF/H1 Antagonist | Neuronal Signaling | Immunology/Inflammation | GPCR/G Protein | Autophagy | Histamine Receptor | Autophagy | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Rupatadine Fumarate 纯度/质量文件 | Rupatadine Fumarate 亚型比较 | Rupatadine Fumarate 生物活性 | Rupatadine Fumarate 参考文献 | Rupatadine Fumarate 实验方案 | Rupatadine Fumarate 技术信息

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