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Terfenadine Sale

(Synonyms: 特非那定; (±)-Terfenadine; MDL-991) 目录号 : GC10978

A selective histamine H1-receptor antagonist

Terfenadine Chemical Structure

Cas No.:50679-08-8

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥452.00
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100mg
¥347.00
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Sample solution is provided at 25 µL, 10mM.

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产品描述

Terfenadine ((±)-Terfenadine) is a potent open-channel blocker of hERG with an IC50 of 204 nM[1]. 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[2].

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[2]. Terfenadine (2-10 μM; 8 hours) induces dose-dependent cytotoxicity[2]. 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[2].

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[3].

References:
[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.

Chemical Properties

Cas No. 50679-08-8 SDF
别名 特非那定; (±)-Terfenadine; MDL-991
化学名 1-(4-tert-butylphenyl)-4-[4-[hydroxy(diphenyl)methyl]piperidin-1-yl]butan-1-ol
Canonical SMILES CC(C)(C)C1=CC=C(C=C1)C(CCCN2CCC(CC2)C(C3=CC=CC=C3)(C4=CC=CC=C4)O)O
分子式 C32H41NO2 分子量 471.67
溶解度 ≥ 18mg/mL in DMSO 储存条件 Store at -20°C
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1 mM 2.1201 mL 10.6006 mL 21.2013 mL
5 mM 0.424 mL 2.1201 mL 4.2403 mL
10 mM 0.212 mL 1.0601 mL 2.1201 mL
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