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/ 组胺受体 / Bepotastine besilate

苯磺酸贝托司汀 /Bepotastine besilate {[allProObj[0].p_purity_real_show]}

货号：A307253 同义名： Bepotastine (besylate);TAU 284

Bepotastine besilate is a selective antagonist of histamine 1 (H1) receptor with pIC50 of 5.7.

Bepotastine besilate 化学结构 CAS号：190786-44-8
Bepotastine besilate 化学结构
CAS号：190786-44-8
Bepotastine besilate 3D分子结构
CAS号：190786-44-8
Bepotastine besilate 化学结构 CAS号：190786-44-8
Bepotastine besilate 3D分子结构 CAS号：190786-44-8
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Bepotastine besilate 纯度/质量文件 产品仅供科研

货号：A307253 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。

Bepotastine besilate 生物活性

靶点

  • H1 receptor

    Histamine H1 receptor, pIC50:5.7
描述 Bepotastine besilate (BB) is a second-generation H1-antihistamine that, as an ophthalmic solution, is approved in the United States by the Food and Drug Administration (FDA) for the treatment of allergic conjunctivitis. BB is effective and well-tolerated in the treatment of allergic rhinitis. Side effects are infrequent in patients with AR who do not have kidney or liver disease[3]. Bepotastine may also have other immunoactive properties, such as inhibition of eosinophil migration, interleukin-5 (IL-5), leukotrienes (e.g., LTB4) and platelet-activating factor (PAF)[4]. Bepotastine in vivo dose-dependently inhibited the acceleration of histamine-induced vascular permeability and inhibited homologous passive cutaneous anaphylaxis in guinea pig studies. In mouse models of itching, oral bepotastine inhibited the frequency and duration of scratching behavior. Multiple in vivo animal toxicology studies have demonstrated bepotastine to be safe with no significant effects on respiratory, circulatory, central nervous, digestive, or urinary systems[5].

Bepotastine besilate 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT02686294 Rhinitis, Allergic, Perennial Phase 1 Completed - Korea, Republic of ... 展开 >> The Korea Univertisy Anam Hospital Seoul, Korea, Republic of, 136-705 收起 <<
NCT02682745 Rhinitis, Allergic, Perennial Phase 1 Completed - Korea, Republic of ... 展开 >> The Korea Univertisy Anam Hospital Seoul, Korea, Republic of, 136-705 收起 <<
NCT03200496 Healthy Phase 1 Completed - Korea, Republic of ... 展开 >> Korea University Anam Hospital Seoul, Korea, Republic of 收起 <<

Bepotastine besilate 参考文献

[1]Ohashi R, Kamikozawa Y, et al. Effect of P-glycoprotein on intestinal absorption and brain penetration of antiallergic agent bepotastine besilate. Drug Metab Dispos. 2006 May;34(5):793-9.

[2]Da Prada M, Kettler R, et al. Neurochemical profile of moclobemide, a short-acting and reversible inhibitor of monoamine oxidase type A. J Pharmacol Exp Ther. 1989 Jan;248(1):400-14.

[3]Carrillo-Martin I, Gonzalez-Estrada A, Dimov V. Bepotastine besilate for the treatment of perennial allergic rhinitis. Expert Opin Pharmacother. 2018 Oct;19(15):1727-1730

[4]Bielory L, Duttachoudhury S, McMunn A. Bepotastine besilate for the treatment of pruritus. Expert Opin Pharmacother. 2013 Dec;14(18):2553-69

[5]Williams JI, Gow JA, Klier SM, McCue SL, Salapatek AM, McNamara TR. Non-clinical pharmacology, pharmacokinetics, and safety findings for the antihistamine bepotastine besilate. Curr Med Res Opin. 2010 Oct;26(10):2329-38

Bepotastine besilate 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.83mL

0.37mL

0.18mL

9.14mL

1.83mL

0.91mL

18.28mL

3.66mL

1.83mL

Bepotastine besilate 技术信息

CAS号190786-44-8
分子式C27H31ClN2O6S
分子量 547.063
别名 Bepotastine (besylate);TAU 284
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Inert atmosphere,Room Temperature
溶解度

DMSO: 105 mg/mL(191.93 mM)，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: Bepotastine | 190786-44-8 | Histamine Receptor | pruritus | Histamine H1 Receptor Antagonist | GPCR/G Protein | Neuronal Signaling | Immunology/Inflammation | Histamine Receptor | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Bepotastine besilate 纯度/质量文件 | Bepotastine besilate 亚型比较 | Bepotastine besilate 生物活性 | Bepotastine besilate 临床数据 | Bepotastine besilate 参考文献 | Bepotastine besilate 实验方案 | Bepotastine besilate 技术信息

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