UC-781

UC-781 (NSC 675186) is a highly potent and selective nonnucleoside reverse transcriptase inhibitor (NNRTI) of HIV-1 with an IC₅₀ value of 5 nM. UC-781 is stable under low PH or various temperatures conditions. UC-781 has antiviral activity and resistance^[1][2][3]. In Vitro: UC-781 (0.05, 0.2 and 0.5 % UC-781 replens gel; 10 d) is released from gel preparation and eliminates HIV-1 virus in CEM cells^[1].
UC-781 (3.75-30 μM) inhibits the growth of Bacillus cereus (about 50 %)^[1].
UC-781 inhibits the activity of HIV-1 (Ⅲ_B) in CEM T cells (EC₅₀=6 nM; IC₅₀=23 nM). UC-781 inhibits the activity of HIV in Monocyte-Derived Dendritic Cell (MO-DC) and autologous CD4⁺ T cells with EC₅₀ values of 550 nM and 1588 nM, respectively^[2].
UC-781 (1 µM or 10 µM; 24 h) effectively prevents or blocks MO-DC and autologous CD4⁺ T cells infected HIV^[2].
UC-781 (0.001-1000 µM; 2 h) inhibits the transition of virus cervical explants infected with HIV-1_BaL^[4].
In Vivo: UC-781 (100 µl 5% UC-781 replens gel; intravaginal; once daily for 10 days) releases from gel preparation and shows low toxicity to normal tissues in female rabbit^[1].