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.

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].

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].

References:
[1]. Balzarini J, et al. Preclinical studies on thiocarboxanilide UC-781 as a virucidal agent. AIDS. 1998 Jul 9;12(10):1129-38.
[2]. Van Herrewege Y, et al. In vitro evaluation of nonnucleoside reverse transcriptase inhibitors UC-781 and TMC120-R147681 as human immunodeficiency virus microbicides. Antimicrob Agents Chemother. 2004 Jan;48(1):337-9.
[3]. Balzarini J, et al. Highly favorable antiviral activity and resistance profile of the novel thiocarboxanilide pentenyloxy ether derivatives UC-781 and UC-82 as inhibitors of human immunodeficiency virus type 1 replication. Mol Pharmacol. 1996 Aug;50(2):394-401.
[4]. Fletcher P, et al. The nonnucleoside reverse transcriptase inhibitor UC-781 inhibits human immunodeficiency virus type 1 infection of human cervical tissue and dissemination by migratory cells. J Virol. 2005 Sep;79(17):11179-86.