| Bioactivity | 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]. | ||||||||||||
| Invitro | 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]. Apoptosis Analysis[2] Cell Line: | ||||||||||||
| Name | Terfenadine | ||||||||||||
| CAS | 50679-08-8 | ||||||||||||
| Formula | C32H41NO2 | ||||||||||||
| Molar Mass | 471.67 | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
|