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首页 / 抑制剂/激动剂 / 膜转运蛋白 / 钾通道 / Terfenadine/特非那定

Terfenadine/特非那定 {[allProObj[0].p_purity_real_show]}

货号：A373035 同义名： MDL-991; NSC 665802

Terfenadine是一种强效的 hERG 开放通道阻滞剂，平均 IC50 值为 204 nM。

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Terfenadine/特非那定 化学结构 CAS号：50679-08-8
Terfenadine/特非那定 化学结构
CAS号：50679-08-8
Terfenadine/特非那定 3D分子结构
CAS号：50679-08-8
Terfenadine/特非那定 化学结构 CAS号：50679-08-8
Terfenadine/特非那定 3D分子结构 CAS号：50679-08-8
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Terfenadine/特非那定 纯度/质量文件 产品仅供科研

货号：A373035 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 Potassium Channel ↓ 其他靶点 纯度
Tolbutamide ✔ 98%
Glimepiride ++++

SUR1, IC50: 5.4 nM

SUR2B, IC50: 7.3 nM

 		97%
Dronedarone HCl ✔ 95%
Gliquidone ++

Potassium channel, IC50: 27.2 nM

 		99%
TRAM-34 +++

IKCa1 (KCa3.1), Kd: 20 nM

 		98%
Glibenclamide ✔ 98%
Amiodarone HCl ✔ 97%
Gliclazide ++

Potassium channel, IC50: 184 nM

 		98%
Repaglinide ✔ 98%
Dofetilide ✔ 98%
Nateglinide ✔ 99%
Quinine HCl dihydrate ✔ 98%
ML133 HCl +

Kir2.1, IC50: 290 nM

 		99%
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。

Terfenadine/特非那定 生物活性

靶点

  • Calcium Channel
描述 Terfenadine is a potent open-channel blocker of hERG with a mean IC50 of 204 nM[3]. Terfenadine inhibited Kir2.3 channels with a strikingly greater potency (IC50 = 1.06 ± 0.11 μmol L-1) compared to Kir2.1 channels (IC50 = 27.8 ± 4.8 μmol L-1). The Kir2.3(I213L) mutant, possessing a larger affinity for phosphatidylinositol 4,5-bisphosphate (PIP2) than the wild-type Kir2.3, was less sensitive to terfenadine inhibition (IC50 = 13.0 ± 2.9 μmol L-1). Additionally, the PIP2 intracellular application had largely reduced the inhibition of Kir2.1 channels by terfenadine[4]. Terfenadine, an H1 histamine receptor antagonist, acts as a potent apoptosis inducer in melanoma cells through modulation of Ca(2+) homeostasis. Terfenadine induced autophagy, that can promote apoptosis[5]. Terfenadine combined with EPI (epirubicin) synergistically inhibits the growth and metastatic processes of resistant cells both in vitro and in vivo[6].

Terfenadine/特非那定 细胞实验

Cell Line
Concentration Treated Time Description References
Human liver microsomes 5, 10, 20, 40, 80, 160 µM 20 minutes To assess the potency of nefazodone, sertraline, and fluoxetine in inhibiting terfenadine biotransformation. Results showed that nefazodone and sertraline were moderately weak inhibitors of terfenadine N-dealkylation (Ki values of 10±4 and 10±3 μM, respectively), while fluoxetine was a very weak inhibitor (Ki value of 68±15 μM). Br J Clin Pharmacol. 1998 Mar;45(3):318-21
Human colorectal cancer HCT116 cells Various concentrations 24 and 48 hours To evaluate the effect of terfenadine on the growth and proliferation of HCT116 cells. Results showed that terfenadine markedly attenuated the viability of HCT116 cells by abrogating histamine H1 receptor (H1R) signaling. Front Pharmacol. 2024 Jun 13;15:1418266
Hs294T human melanoma cells 9.9 µM (IC50) 24 hours To study the cytotoxic effect of Terfenadine on Hs294T melanoma cells in complete medium, results showed that Terfenadine induced dose-dependent apoptosis. Apoptosis. 2011 Dec;16(12):1253-67
HT144 human melanoma cells 9.6 µM (IC50) 24 hours To study the cytotoxic effect of Terfenadine on HT144 melanoma cells in complete medium, results showed that Terfenadine induced dose-dependent apoptosis. Apoptosis. 2011 Dec;16(12):1253-67
A375 human melanoma cells 10.4 µM (IC50) 24 hours To study the cytotoxic effect of Terfenadine on A375 melanoma cells in complete medium, results showed that Terfenadine induced dose-dependent apoptosis. Apoptosis. 2011 Dec;16(12):1253-67
Cardiomyocytes 5-10 µM 24 hours Induced cardiomyocyte apoptosis and ventricular dilation Korean Circ J. 2017 Nov;47(6):960-969
Mutant hERG channels (T623A, S624A, Y652A, F656A) 3.5 µM 5 seconds To determine the effect of mutations on terfenadine block, results showed that T623A, S624A, Y652A, F656A mutations reduced channel sensitivity to terfenadine J Pharmacol Sci. 2008 Nov;108(3):301-7
Wild-type hERG channels 350 nM 5 seconds To determine the blocking effect of terfenadine on hERG channels, results showed an IC50 of 350 nM J Pharmacol Sci. 2008 Nov;108(3):301-7
A2780-ADR cells 2.5 to 10 µM 6 hours Terfenadine restores doxorubicin sensitivity in drug-resistant ovarian cancer cells by inhibiting CaMKII/CREB1-mediated ABCB1 expression. Front Oncol. 2022 Nov 10;12:1068443
A375 human melanoma cells 6.8 µM (IC50) 8 hours To study the cytotoxic effect of Terfenadine on A375 melanoma cells under serum-free conditions, results showed that starvation enhanced the cytotoxic effect of Terfenadine. Apoptosis. 2011 Dec;16(12):1253-67

Terfenadine/特非那定 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
BALB/c nude mice HCT116 tumor xenograft model Intraperitoneal injection 2 mg/kg and 10 mg/kg Once daily for 20 days To evaluate the inhibitory effect of terfenadine on the growth of HCT116 tumor xenografts in vivo. Results showed that terfenadine (10 mg/kg) substantially retarded the growth of HCT116 tumor xenografts. Front Pharmacol. 2024 Jun 13;15:1418266
Dog Chronic atrioventricular block dog model Oral 3 or 30 mg/kg Single dose To evaluate the proarrhythmic effects of terfenadine in chronic atrioventricular block dogs. Results showed that the high dose significantly prolonged QT interval and induced torsades de pointes (TdP) in the 4-6 weeks model group. Cell Death Dis. 2017 Jul 6;8(7):e2913
Dog Chronic atrioventricular block dog model Oral 3 or 30 mg/kg Single dose To evaluate the proarrhythmic effects of terfenadine in chronic atrioventricular block dogs. Results showed that the high dose significantly prolonged QT interval and induced torsades de pointes (TdP) in the 4-6 weeks model group. Br J Pharmacol. 2006 Mar;147(6):634-41
Zebrafish Zebrafish dilated cardiomyopathy model Immersion 5-10 µM, 35-45 µM 24 hours (low dose), 1 hour (moderate dose) Induced dilated cardiomyopathy, characterized by ventricular dilation, reduced cardiac contractility, and cardiomyocyte apoptosis Korean Circ J. 2017 Nov;47(6):960-969

Terfenadine/特非那定 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
NCT01940393 Urticaria Phase 4 Completed - Colombia ... 展开 >> Medellin Medellin, Antioquia, Colombia 收起 <<
NCT02056743 Healthy Phase 1 Completed - Korea, Republic of ... 展开 >> Clinical Trial Center of Chonbuk National University Hospital Jeonju, Jeollabuk-do, Korea, Republic of 收起 <<
NCT02966665 Chronic Obstructive Pulmonary ... 展开 >>Disease Pulmonary Artery Hypertension Heart Failure Hypertension 收起 << Phase 1 Recruiting August 2020 United States, Utah ... 展开 >> George E Wahlen VA Medical Center Recruiting Salt Lake City, Utah, United States, 84132 Contact: Russell Richardson, Ph.D.    801-582-1565    r.richardson@hsc.utah.edu    Contact: Ashley Nelson, MD    801-582-1565 ext 4127    ash.nelson@hsc.utah.edu 收起 <<

Terfenadine/特非那定 参考文献

[1]Nicolau-Galmes F, Asumendi A, et al. Terfenadine induces apoptosis and autophagy in melanoma cells through ROS-dependent and -independent mechanisms. Apoptosis. 2011 Dec;16(12):1253-67.

[2]Kamiya K, Niwa R, et al. Molecular determinants of hERG channel block by terfenadine and cisapride. J Pharmacol Sci. 2008 Nov;108(3):301-7. Epub 2008 Nov 6.

[3]Kamiya K, Niwa R, Morishima M, Honjo H, Sanguinetti MC. Molecular determinants of hERG channel block by terfenadine and cisapride. J Pharmacol Sci. 2008 Nov;108(3):301-7

[4]Delgado-Ramírez M, Rodriguez-Leal FJ, Rodríguez-Menchaca AA, Moreno-Galindo EG, Sanchez-Chapula JA, Ferrer T. Inhibitory effect of terfenadine on Kir2.1 and Kir2.3 channels. Acta Pharm. 2021 Jun 1;71(2):317-324

[5]Nicolau-Galmés F, Asumendi A, Alonso-Tejerina E, Pérez-Yarza G, Jangi SM, Gardeazabal J, Arroyo-Berdugo Y, Careaga JM, Díaz-Ramón JL, Apraiz A, Boyano MD. Terfenadine induces apoptosis and autophagy in melanoma cells through ROS-dependent and -independent mechanisms. Apoptosis. 2011 Dec;16(12):1253-67

[6]An L, Li DD, Chu HX, Zhang Q, Wang CL, Fan YH, Song Q, Ma HD, Feng F, Zhao QC. Terfenadine combined with epirubicin impedes the chemo-resistant human non-small cell lung cancer both in vitro and in vivo through EMT and Notch reversal. Pharmacol Res. 2017 Oct;124:105-115

Terfenadine/特非那定 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.12mL

0.42mL

0.21mL

10.60mL

2.12mL

1.06mL

21.20mL

4.24mL

2.12mL

Terfenadine/特非那定 技术信息

CAS号50679-08-8
分子式C32H41NO2
分子量 471.67
SMILES Code CC(C)(C1=CC=C(C(CCCN2CCC(C(C3=CC=CC=C3)(O)C4=CC=CC=C4)CC2)O)C=C1)C
MDL No. MFCD00079622
别名 MDL-991; NSC 665802; Terfen; Seldane; BRN 5857899; DL-Terfenadine; MDL 9918; (±)-Terfenadine
运输蓝冰
InChI Key GUGOEEXESWIERI-UHFFFAOYSA-N
Pubchem ID 5405
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Sealed in dry,2-8°C
溶解方案

DMSO: 50 mg/mL(106.01 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
方案 三

Tags: Terfenadine | MDL-991;NSC 665802;Terfen;Seldane;BRN 5857899;DL-Terfenadine;MDL 9918;(±)-Terfenadine | Potassium Channel | AmBeed-信号通路专用抑制剂 | Terfenadine/特非那定 纯度/质量文件 | Terfenadine/特非那定 亚型比较 | Terfenadine/特非那定 生物活性 | Terfenadine/特非那定 临床数据 | Terfenadine/特非那定 参考文献 | Terfenadine/特非那定 实验方案 | Terfenadine/特非那定 技术信息

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