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/ 组胺受体 / Fexofenadine HCl

盐酸非索非那定 /Fexofenadine HCl {[allProObj[0].p_purity_real_show]}

货号：A304995 同义名： MDL-16455 hydrochloride;Terfenadine carboxylate hydrochloride

Fexofenadine inhibits histamine H1 receptor with IC50 of 246 nM.

Fexofenadine HCl 化学结构 CAS号：153439-40-8
Fexofenadine HCl 化学结构
CAS号：153439-40-8
Fexofenadine HCl 3D分子结构
CAS号：153439-40-8
Fexofenadine HCl 化学结构 CAS号：153439-40-8
Fexofenadine HCl 3D分子结构 CAS号：153439-40-8
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Fexofenadine HCl 纯度/质量文件 产品仅供科研

货号：A304995 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 ✔ 99%
Betahistine +

Histamine H3 receptor, IC50: 1.9 μM

 		98%
Ciproxifan maleate +++

Histamine H3 receptor, IC50: 9.2 nM

 		99%+
S 38093 ++

rat H3 receptor, Ki: 1.44 μM

human H3 receptor, Ki: 1.2 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。

Fexofenadine HCl 生物活性

靶点

  • H1 receptor

    Histamine H1 receptor, IC50:246 nM
描述 Fexofenadine HCl is the acid metabolite of terfenadine (Seldane). fexofenadine HCl has no significant effect on QTc(corrected QT interval), even at doses > 10-fold higher than that is efficacious for SAR(seasonal allergic rhinitis) [3]. Fexofenadine is a highly specific, H1-receptor antagonist with a safety profile similar to placebo. Fexofenadine has a high margin of safety and is also well tolerated in subjects with renal or hepatic impairment, in children and the elderly. The recommended dose of fexofenadine HC1 is 120 mg daily for SAR (either as 120 mg once daily or 60 mg twice daily) or 180 mg once daily for CIU[4]. Fexofenadine is highly selective for peripheral H(1)-receptors and does not cross the blood-brain barrier. Fexofenadine has also been shown to have a favorable effect on nasal congestion. This therapeutic advantage might be related to its significant antiallergic properties, ie, the demonstrated ability of fexofenadine to blunt the inflammatory effects of preformed and de novo synthesized mediators at clinically relevant doses in vivo and in vitro[5].

Fexofenadine HCl 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
NCT01375790 Aging Phase 3 Completed - Spain ... 展开 >> Albada Centre Socio Sanitari Parc Taulí Sabadell, Babadell, Spain, 08208 Ballesol Badalona Badalona, Barcelona, Spain, 08911 Ballesol Barberà Barberà del Vallès, Barcelona, Spain, 08210 Residència Allegra Sabadell, Barcelona, Spain, 08203 Residència Poble Nou Barcelona, Spain, 08005 Ballesol Fabra i Puig Barcelona, Spain, 08016 Ballesol Almogàvers Barcelona, Spain, 08018 Residència Mapfre Quavitae Barcelona, Spain, 08025 Residència AMMA Horta Barcelona, Spain, 08035 Residència Collserola (Mutuam) Barcelona, Spain, 08035 收起 <<
NCT02796898 Prostate Cancer ... 展开 >> Rising Prostate Specific Antigen (PSA) 收起 << Phase 1 Phase 2 Recruiting December 31, 2019 United States, New Jersey ... 展开 >> AdvanceMed Research Completed Lawrence, New Jersey, United States, 08648 United States, New York Montefiore Medical Center- Montefiore Medical Park Not yet recruiting Bronx, New York, United States, 10461 Contact: Gartrell Benjamin, MD    718-405-8404    bgartrel@montefiore.org    Eastchester Center for Cancer Care Recruiting Bronx, New York, United States, 10469 Contact: Carmen Vicuna    718-732-4078    cvicuna@nycancer.com    AccuMed Research Associates Recruiting Garden City, New York, United States, 11530-1664 Contact: Tammi Allegra, RN    516-746-2190    tallegra.accumedresearch@gmail.com    United States, Pennsylvania MidLantic Urology Recruiting Bala-Cynwyd, Pennsylvania, United States, 19004 Contact: Cheryl A Zinar, RN, BSN    610-667-0458       Principal Investigator: Laurence H Belkoff, DO 收起 <<
NCT00078195 Hay Fever Hyp... 展开 >>ersensitivity Allergy Rhinitis 收起 << Phase 2 Completed - United States, Iowa ... 展开 >> University of Iowa Iowa City, Iowa, United States, 52242 United States, Nebraska Creighton University Omaha, Nebraska, United States, 68131 United States, Wisconsin University of Wisconsin Madison, Wisconsin, United States, 53705 收起 <<

Fexofenadine HCl 参考文献

[1]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.

[2]Petri N, Tannergren C, et al. Transport characteristics of fexofenadine in the Caco-2 cell model. Pharm Res. 2004 Aug;21(8):1398-404.

[3]Pratt CM, Mason J, Russell T, Reynolds R, Ahlbrandt R. Cardiovascular safety of fexofenadine HCl. Am J Cardiol. 1999 May 15;83(10):1451-4

[4]Mason J, Reynolds R, Rao N. The systemic safety of fexofenadine HCl. Clin Exp Allergy. 1999 Jul;29 Suppl 3:163-70; discussion 171-3

[5]Meeves SG, Appajosyula S. Efficacy and safety profile of fexofenadine HCl: a unique therapeutic option in H1-receptor antagonist treatment. J Allergy Clin Immunol. 2003 Oct;112(4 Suppl):S69-77

Fexofenadine HCl 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.86mL

0.37mL

0.19mL

9.29mL

1.86mL

0.93mL

18.58mL

3.72mL

1.86mL

Fexofenadine HCl 技术信息

CAS号153439-40-8
分子式C32H40ClNO4
分子量 538.117
别名 MDL-16455 hydrochloride;Terfenadine carboxylate hydrochloride;Fexofenadine (hydrochloride);MDL 16455A;Fexofenadine hydrochloride
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,Store in freezer, under -20°C
溶解度

DMSO: 105 mg/mL(195.12 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: Fexofenadine | 153439-40-8 | MDL-16455 | Terfenadine carboxylate | MDL16455 | MDL 16455 | H1R 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 | Fexofenadine HCl 纯度/质量文件 | Fexofenadine HCl 亚型比较 | Fexofenadine HCl 生物活性 | Fexofenadine HCl 临床数据 | Fexofenadine HCl 参考文献 | Fexofenadine HCl 实验方案 | Fexofenadine HCl 技术信息

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