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比拉斯汀 /Bilastine {[allProObj[0].p_purity_real_show]}

货号:A325945 同义名: F-96221-BM1

Bilastine selectively antagonizes histamine H1 receptor and it is used to treat allergic rhinoconjunctivitis and urticaria.

Bilastine 化学结构 CAS号:202189-78-4
Bilastine 化学结构
CAS号:202189-78-4
Bilastine 3D分子结构
CAS号:202189-78-4
Bilastine 化学结构 CAS号:202189-78-4
Bilastine 3D分子结构 CAS号:202189-78-4
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Bilastine 纯度/质量文件 产品仅供科研

货号:A325945 标准纯度: {[allProObj[0].p_purity_real_show]}
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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。

Bilastine 生物活性

靶点
  • H1 receptor

    H1 receptor, Ki:44.15 nM

描述 Bilastine is a potent and highly selective H1-antihistamine approved for the treatment of allergic rhinoconjunctivitis and urticaria. Bilastine is a suitable option for the treatment of patients with allergic rhinoconjunctivitis or urticaria across age groups from school-age children to elderly patients[3]. Bilastine, a novel new-generation antihistamine that is highly selective for the H1 histamine receptor, has a rapid onset and prolonged duration of action. Bilastine is generally well tolerated, both at standard and at supratherapeutic doses, appears to have less sedative potential than other second-generation antihistamines, and has no cardiotoxicity[4]. Bilastine 20 mg once daily (therapeutic dose) is non-sedating, does not enhance the effects of alcohol or CNS sedatives, does not impair driving performance and has at least similar efficacy as other second-generation H1-antihistamines in the treatment of allergic rhinoconjunctivitis and urticaria[5]. With respect to somnolence, bilastine is a substrate for P-glycoprotein, a membrane pump which prevents it crossing the blood-brain barrier[6].

Bilastine 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
NCT02557269 Seasonal Allergic Rhinitis Phase 4 Unknown December 2015 Bulgaria ... 展开 >> Medical University Sofia, University Hospital "Alexandrovska", Clinic of Allergy and Asthma Sofia, Bulgaria, 1431 收起 <<
NCT01940393 Urticaria Phase 4 Completed - Colombia ... 展开 >> Medellin Medellin, Antioquia, Colombia 收起 <<
NCT00421109 Urticaria Phase 3 Completed - -

Bilastine 参考文献

[1]Jauregizar N, de la Fuente L, et al. Pharmacokinetic-pharmacodynamic modelling of the antihistaminic (H1) effect of bilastine. Clin Pharmacokinet. 2009;48(8):543-54.

[2]Corcostegui R, Labeaga L, et al. Preclinical pharmacology of bilastine, a new selective histamine H1 receptor antagonist: receptor selectivity and in vitro antihistaminic activity. Drugs R D. 2005;6(6):371-84.

[3]Church MK, Tiongco-Recto M, Ridolo E, Novák Z. Bilastine: a lifetime companion for the treatment of allergies. Curr Med Res Opin. 2020 Mar;36(3):445-454

[4]Wang XY, Lim-Jurado M, Prepageran N, Tantilipikorn P, Wang de Y. Treatment of allergic rhinitis and urticaria: a review of the newest antihistamine drug bilastine. Ther Clin Risk Manag. 2016 Apr 13;12:585-97

[5]Jáuregui I, Ramaekers JG, Yanai K, Farré M, Redondo E, Valiente R, Labeaga L. Bilastine: a new antihistamine with an optimal benefit-to-risk ratio for safety during driving. Expert Opin Drug Saf. 2016 Jan;15(1):89-98

[6]Church MK, Labeaga L. Bilastine: a new H1 -antihistamine with an optimal profile for updosing in urticaria. J Eur Acad Dermatol Venereol. 2017 Sep;31(9):1447-1452

Bilastine 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.16mL

0.43mL

0.22mL

10.78mL

2.16mL

1.08mL

21.57mL

4.31mL

2.16mL

Bilastine 技术信息

CAS号202189-78-4
分子式C28H37N3O3
分子量 463.612
别名 F-96221-BM1
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: 9 mg/mL(19.41 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
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