Terfenadine

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Terfenadine 是一种组胺 H1 受体拮抗剂，可阻断 HERG 和 KATP (KIR6) 通道。

Terfenadine is a histamine H1-receptor antagonist, which blocks HERG and KATP (KIR6) channels. (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.

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 AssayCell 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.

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.

MDL 9918 | NSC 665802 | (±)-Terfenadine | DL-Terfenadine

Endocrinology/Hormones

5-HT Receptor

HT| mAChR| Potassium Channel

Inflammation/Immunology

——

50679-08-8

471.67

C32H41NO2

>98% (HPLC)

Water: 0.0963 mg/L

OC(C1=CC=C(C(C)(C)C)C=C1)CCCN2CCC(C(C3=CC=CC=C3)(O)C4=CC=CC=C4)CC2

1-(4-(tert-butyl)phenyl)-4-(4-(hydroxydiphenylmethyl)piperidin-1-yl)butan-1-ol

(-20℃)

With Ice Pack

≥ 2 years