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Terfenadine

CAS No. : 50679-08-8

MCE 站：Terfenadine

产品活性：Terfenadine ((±)-Terfenadine) 是一种有效的 hERG 开放通道抑制剂, IC₅₀为 204 nM。Terfenadine 也是一种 H1 组胺受体 (histamine receptor) 拮抗剂，通过调节 Ca²⁺ 稳态在黑素瘤细胞中起到有效的细胞凋亡诱导作用。 Terfenadine 诱导 ROS 依赖性细胞凋亡，同时激活 Caspase-4，-2，-9。

研究领域：Membrane Transporter/Ion Channel  |  Immunology/Inflammation  |  GPCR/G Protein  |  Neuronal Signaling  |  Apoptosis

作用靶点：Potassium Channel  |  Histamine Receptor  |  Na+/Ca2+ Exchanger  |  Caspase  |  Apoptosis

In Vitro: 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.

In Vivo: 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.

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