Terfenadine-racemic-Terfenadine-DataSheet-生命科學試劑-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemETerfenadineCat. No.: HY-B1193CAS No.: 50679-08-8Synonyms: ()-Terfenadine; MDL-991分式: CHNO分量: 471.67作靶點: Potassium Channel; Histamine Receptor; Na+/Ca2+Exchanger; ROS; Caspase; Apoptosis作通路: Membrane Transporter/Ion Channel; GPCR

2、/G Protein;Immunology/Inflammation; Neuronal Signaling; Protein Tyrosine Kinase/RTK; Apoptosis儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數據體外實驗 DMSO : 50 mg/mL (106.01 mM)H2O : 40% PEG300 5% Tween-80 45% saline1/3 Master of Small Molecules 您邊的抑制劑師www.MedChemESolubility:

3、 2.5 mg/mL (5.30 mM); Clear solution2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (5.30 mM); Clear solution3. 請依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (5.30 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Terfenadine ()-Terfenadine)種有效的 hERG 開放通道抑制劑, IC50為 204 nM。Terf

4、enadine 也 種H1 組胺受體 (histamine receptor) 拮抗劑，通過調節(jié) Ca2+ 穩(wěn)態(tài)在素瘤細胞中起到有效的細胞凋亡誘導作。 Terfenadine 誘導 ROS 依賴性細胞凋亡，同時激活 Caspase-4，-2，-9，誘導 p73，Noxa。IC50 & Target H1 receptor Caspase-4 Caspase-2 Caspase-9體外研究Terfenadine ()-Terfenadine) (4-20 M; 24 hours) induces dose and time-dependent apoptosis on A375melanoma

5、cells. The IC50 after 24 h of TEF treatment in complete medium was 10.4 M for A375 cells, 9.9 M for Hs294T cells and 9.6 for HT144 cells 2.Terfenadine (2-10 M; 8 hours) induces dose-dependent cytotoxicity 2.Terfenadine (10 M; 8 hours) causes a massive vacuolization of the cytoplasm and autophagic va

6、cuoles ofboth double and multiple membranes and at various stages. Terfenadine induces autophagy by ROS-dependent and -independent mechanisms 2.Terfenadine (10 M; 8-28 hours) increases p53, p73, p21 and Noxa protein levels in cells in completemedium 2.Apoptosis Analysis 2Cell Line: A375, HT144 and H

7、s294T cellsConcentration: 4, 8, 12, 16, 20 MIncubation Time: 24 hoursResult: Induced dose and time-dependent apoptosis.Cell Cytotoxicity Assay 2Cell Line: A375 melanoma cellsConcentration: 2, 4, 6, 8, 10 MIncubation Time: 8 hoursResult: Induces dose-dependent cytotoxicity.Cell Autophagy Assay 22/3 M

8、aster of Small Molecules 您邊的抑制劑師www.MedChemECell Line: A375 cellsConcentration: 10 MIncubation Time: 8 hoursResult: Caused a massive vacuolization of the cytoplasm and autophagic vacuoles of bothdouble and multiple membranes and at various stages.Western Blot Analysis 2Cell Line: A375 cellsConcentra

9、tion: 10 MIncubation Time: 8, 16, 28 hoursResult: Increase p53, p73, p21 and Noxa protein levels.體內研究 Terfenadine (p.o.; 40 mg/kg; for 16 days) produces a significant inhibition of tumour growth rate andenhances the anti-cancer effect of EPI in chemo-resistant NSCLC xenograft models 3.Animal Model:

10、6-week-old male BALB/cA-nu mice 3Dosage: 40 mg/kgAdministration: P.o.; for 16 daysResult: Produced a significant inhibition of tumour growth rate.REFERENCES1. Kamiya K, et al. Molecular determinants of hERG channel block by terfenadine and cisapride. J Pharmacol Sci. 2008 Nov;108(3):301-307.2. Nicol

11、au-Galms F, et al. Terfenadine induces apoptosis and autophagy in melanoma cells through ROS-dependent and -independentmechanisms. 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 invivo through EMT and Notch reversal. Pharmacol Res. 2017 Oct;124:105-115.McePdfHeightCaution: Product has