产品
编 号：F372526
分子式：C32H41NO2
分子量：471.67
分子式：C32H41NO2
分子量：471.67
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
100mg
400
In-stock
结构图
CAS No: 50679-08-8
产品详情
生物活性：
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.
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.
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.
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.
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.
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.
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