货号	规格	价格	上海	北京	武汉	南京
S80760-25mg	98%	￥130.00 S80760-25mg ￥130.00 现货	3 3	-	-	-
S80760-100mg	98%	￥220.00 S80760-100mg ￥220.00 现货	1 1	-	-	-
S80760-500mg	98%	￥650.00 S80760-500mg ￥650.00 现货	2 2	-	-	-

产品介绍

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

产品描述：

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。

参考文献(2篇)

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

质检证书(COA)

输入产品批号：

如何获取质检证书(COA)?

请输入货号和一个与之匹配的批号。
例如:
批号：JS298415 货号：S20001-25g
在货品标签上如何找到货号和批号?

摩尔浓度计算器

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

质量

浓度

体积

分子摩尔量

计算重置

Terfenadine