244767-67-7

Dapivirine (TMC120) 是二芳基嘧啶 (DAPY) 的原型，是具有口服活性的非核苷类逆转录酶抑制剂 (NRTI)。Dapivirine (TMC120) 可直接与 HIV 的逆转录酶结合。Dapivirine (TMC120)调节自噬并诱导 Akt、Bad 和 SAPK/JNK 的激活。

Dapivirine (4-64 μM, 24, 48, 72, 96 and 120 hours) inhibits proliferation of glioma cells and induces apoptosis (16 μM, 12-48 h)[1].
Dapivirine (8 and 16 μM, 12 h) enhances invasion of glioma cells[1].
Dapivirine (16 μM, 12 h, 24 h and 48 h) promotes autophagy in U87 cells[1].
Dapivirine (TMC120-R147681) apparently blocks infection in the primary cultures at a 10 nM concentration, but secondary cultures revealed that a 100 nM concentration was needed to completely prevent proviral integration[3].

Dapivirine (16 mg/kg, once every 3 days for 12 days) exhibits potent antitumor activity in human glioblastoma models in mice[1].
Dapivirine has been shown to have a half-life in the range of 65 to 90 h[4].