• 产品描述： Terfenadine ((±)-Terfenadine) is a potent open-channel blocker of hERG with an IC50 of 204 nM. Terfenadine, an H1 histamine receptor antagonist, acts as a potent apoptosis inducer in melanoma cells through modulation of Ca2+ homeostasis. Terfenadine induces ROS-dependent apoptosis, simultaneously activates Caspase-4, -2, -9

• 靶点： H1 Receptor;Caspase-4;Caspase-2;Caspase-9;Apoptosis;PotassiumChannel;5-HTReceptor;Caspase;Na+/Ca2+Exchanger;HER;AChR;HistamineReceptor

• 体外研究：
  Terfenadine ((±)-Terfenadine) (4-20 μM; 24 hours) induces dose and time-dependent apoptosis on A375 melanoma cells. The IC50 after 24 h of TEF treatment in complete medium was 10.4 μM for A375 cells, 9.9 μM for Hs294T cells and 9.6 for HT144 cells. Terfenadine (2-10 μM; 8 hours) induces dose-dependent cytotoxicity. Terfenadine (10 μM; 8 hours) causes a massive vacuolization of the cytoplasm and autophagic vacuoles of both double and multiple membranes and at various stages. Terfenadine induces autophagy by ROS-dependent and -independent mechanisms. Apoptosis Analysis Cell Line: A375, HT144 and Hs294T cells Concentration: 4, 8, 12, 16, 20 μM Incubation Time: 24 hours Result: Induced dose and time-dependent apoptosis. Cell Cytotoxicity Assay Cell Line: A375 melanoma cells Concentration: 2, 4, 6, 8, 10 μM Incubation Time: 8 hours Result: Induces dose-dependent cytotoxicity. Cell Autophagy Assay Cell Line: A375 cells Concentration: 10 μM Incubation Time: 8 hours Result: Caused a massive vacuolization of the cytoplasm and autophagic vacuoles of both double and multiple membranes and at various stages.

• 体内研究：
  Terfenadine (p.o.; 40 mg/kg; for 16 days) produces a significant inhibition of tumour growth rate and enhances the anti-cancer effect of EPI in chemo-resistant NSCLC xenograft models. Animal Model: 6-week-old male BALB/cA-nu mice Dosage: 40 mg/kg Administration: P.o.; for 16 days Result: Produced a significant inhibition of tumour growth rate.

• 参考文献：
  1. Kamiya K, et al. Molecular determinants of hERG channel block by terfenadine and cisapride. J Pharmacol Sci. 2008 Nov;108(3):301-307. 2. Nicolau-Galmés F, et al. Terfenadine induces apoptosis and autophagy in melanoma cells through ROS-dependent and -independent mechanisms. Apoptosis. 2011 Dec;16(12):1253-67. 3. An L, et al. 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.

• 溶解性： Soluble  in  DMSO、H2O

• 保存条件： 2-8℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	2.12 ml	10.601 ml	21.201 ml
  5 mM	0.424 ml	2.12 ml	4.24 ml
  10 mM	0.212 ml	1.06 ml	2.12 ml
  50 mM	0.042 ml	0.212 ml	0.424 ml

• 注意：部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

• 2. [IF=3.935] Yixuan Cui et al."A fast and simple approach for the quantification of five anti-hypersensitivity drugs in saliva and urine by portable ion mobility spectrometry based on magnetic graphene oxide dispersive solid phase extraction."J Pharmaceut Biomed. 2020

• 1. Yixuan Cui, Di Liu, Mengqiang Zhao, Junmei Li, Yuke Yang, Mengjiao Li, Jinglin Gao, Ye Jiang, A fast and simple approach for the quantification of five anti-hypersensitivity drugs in saliva and urine by portable ion mobility spectrometry based on magnetic

输入产品批号：

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *