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Terfenadine

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Chemical Structure| 50679-08-8 同义名 : MDL-991;NSC 665802;Terfen;Seldane;BRN 5857899;DL-Terfenadine;MDL 9918;(±)-Terfenadine
CAS号 : 50679-08-8
货号 : A373035
分子式 : C32H41NO2
纯度 : 98%
分子量 : 471.673
MDL号 : MFCD00079622
存储条件：

粉末 Sealed in dry,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

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
动物实验配方：
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].
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 <<
实验方案
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
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