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/ 组胺受体 / Fexofenadine HCl/盐酸非索非那定

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

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

Fexofenadine HCl是一种组胺H1受体拮抗剂，IC50值为246 nM。

Fexofenadine HCl/盐酸非索非那定 化学结构 CAS号：153439-40-8
Fexofenadine HCl/盐酸非索非那定 化学结构
CAS号：153439-40-8
Fexofenadine HCl/盐酸非索非那定 3D分子结构
CAS号：153439-40-8
Fexofenadine HCl/盐酸非索非那定 化学结构 CAS号：153439-40-8
Fexofenadine HCl/盐酸非索非那定 3D分子结构 CAS号：153439-40-8
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Fexofenadine HCl/盐酸非索非那定 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 2HCl ✔ 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 ✔ 96%
Betahistine +

Histamine H3 receptor, IC50: 1.9 μM

 		99%
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

 		99%
Azelastine HCl ✔ 98%
Epinastine HCl ✔ 99%
Levodropropizine ✔ 97%
Cyproheptadine HCl ✔ 98%
Hesperetin ✔ 97%
Olopatadine HCl ✔ 98%
Mianserin HCl ✔ 99+%
Buclizine 2HCl ✔ 95%
Latrepirdine 2HCl ✔ GluR 99%
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/盐酸非索非那定 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/盐酸非索非那定 细胞实验

Cell Line
Concentration Treated Time Description References
Bone-marrow-derived macrophages (BMDMs) 10 µM 24 hours To study the inhibitory effect of Fexofenadine on TNF-α-activated NF-κB pathway and its downstream genes Ann Rheum Dis. 2019 Nov;78(11):1524-1535.
HEK 293 cells 1 mM 24 hours To investigate the effect of fexofenadine on the processing and trafficking of K897T HERG protein. Results showed that fexofenadine did not alter the processing and trafficking of K897T HERG protein. Br J Pharmacol. 2002 Nov;137(6):892-900.
Human NP cells 10 µM 48 hours FFD significantly reduced TNF-α-induced COX-2 and MMP-13 protein expression Front Cell Dev Biol. 2021 Aug 24;9:687024.
Mouse NP cells 10 µM 48 hours FFD significantly reduced TNF-α-induced COX-2 and MMP-13 protein expression Front Cell Dev Biol. 2021 Aug 24;9:687024.

Fexofenadine HCl/盐酸非索非那定 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
C57BL/6 mice DSS-induced inflammatory bowel disease model Oral 0.4, 2, 10 mg/kg Daily administration for 10 days To evaluate the therapeutic effects of Fexofenadine on DSS-induced inflammatory bowel disease. Results showed that Fexofenadine mitigated clinical symptoms, decreased secretions of the proinflammatory cytokine IL-6 and IL-1β, and lowered intestinal inflammation. Int J Mol Sci. 2021 Oct 15;22(20):11155
Mice TNF transgenic mice Oral 10 mg/kg Once daily for 13 weeks To evaluate the preventive and therapeutic effects of Fexofenadine on spontaneous inflammatory arthritis in TNF transgenic mice Ann Rheum Dis. 2019 Nov;78(11):1524-1535.
Sprague-Dawley rats Tail injury model Intraperitoneal injection 10 mg/kg Every other day FFD significantly reversed cartilage tissue loss caused by the tail injury model Front Cell Dev Biol. 2021 Aug 24;9:687024.
BALB/cAJcl mice Pd-induced allergic contact dermatitis (ACD) mice Oral 10 mg/kg Administered once daily at 1 h before each challenge until the end of the experiment To evaluate the suppressive effect of fexofenadine on Pd-induced allergic contact dermatitis, results showed that fexofenadine significantly suppressed footpad swelling and T cell numbers. Int J Mol Sci. 2017 Jun 25;18(7):1357
Wistar albino rats Carrageenan-induced paw edema model Oral 15.87 mg/kg Single dose, observed for 6 hours Evaluate the anti-inflammatory effect of fexofenadine cubosomes. Results showed that cubosomal encapsulation significantly enhanced the in vivo anti-inflammatory efficacy of fexofenadine. Int J Nanomedicine. 2022 Aug 10;17:3543-3560
Mice 6-OHDA model and α-synuclein preformed fibrils (PFF) injection model Oral gavage 20 mg/kg Once daily for 3 weeks (6-OHDA model) or 4 weeks (PFF model) Fexofenadine ameliorated dopaminergic neuronal cell death and motor behavior deficits in the 6-OHDA model and reduced α-syn propagation and neuroinflammation in the PFF model. J Neuroinflammation. 2024 Feb 21;21(1):53
Wistar rats Single pass intestinal absorption model Intestinal perfusion 5 mg/mL 20 min equilibration followed by 90 min perfusion period To evaluate the effect of solid dispersions on intestinal absorption of fexofenadine, results showed significant improvement in drug absorption from solid dispersions Pharmaceutics. 2021 Feb 27;13(3):310
Rabbits Allergic rhinitis model Oral 6 mg/kg Single dose, duration of 8 hours To evaluate the improvement of oral bioavailability of fexofenadine by the optimized formulation. Results showed that the relative bioavailability of the optimized formulation was 125%, significantly increasing blood concentration and absorption rate. Pharmaceutics. 2020 Apr 29;12(5):409

Fexofenadine HCl/盐酸非索非那定 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/盐酸非索非那定 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/盐酸非索非那定 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/盐酸非索非那定 技术信息

CAS号153439-40-8
分子式C32H40ClNO4
分子量 538.12
SMILES Code CC(C)(C1=CC=C(C(O)CCCN2CCC(C(C3=CC=CC=C3)(O)C4=CC=CC=C4)CC2)C=C1)C(O)=O.[H]Cl
MDL No. MFCD00865710
别名 MDL-16455 hydrochloride; Terfenadine carboxylate hydrochloride; MDL 16455A; Fexofenadine hydrochloride
运输蓝冰
InChI Key RRJFVPUCXDGFJB-UHFFFAOYSA-N
Pubchem ID 63002
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Inert atmosphere, store in freezer, under -20°C
溶解方案

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

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议现用现配，当天使用； 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶
方案 一
方案 二

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/盐酸非索非那定 纯度/质量文件 | Fexofenadine HCl/盐酸非索非那定 亚型比较 | Fexofenadine HCl/盐酸非索非那定 生物活性 | Fexofenadine HCl/盐酸非索非那定 临床数据 | Fexofenadine HCl/盐酸非索非那定 参考文献 | Fexofenadine HCl/盐酸非索非那定 实验方案 | Fexofenadine HCl/盐酸非索非那定 技术信息

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