| Description | UC-781 (NSC-675186) is a potent and selective inhibitor of human immunodeficiency virus HIV-1 non-nucleoside reverse transcriptase (NNRTI) I with a C50 value of 5 nM.UC-781 exhibits both antiviral activity and drug resistance.UC-781 is in a stable state, and is unaffected by lower pH or varying temperatures. |
| In vitro | UC-781 (0.05, 0.2, and 0.5 % UC-781 supplemented gel; 10 days) is released from the gel formulation and clears HIV-1 from CEM cells [1].UC-781 (3.75 -30 μM) inhibits the growth of Bacillus cereus (approximately 50%).[1] UC-781 inhibits HIV-1 (IIIB) activity in CEM T cells (EC50=6 nM; IC50=23 nM). UC-781 inhibits HIV activity in monocyte-derived dendritic cells (MO-DCs) and autologous CD4+ T cells with EC50 values of 550 nM and 1588 nM, respectively.[2] UC-781 (1000 nM; 24 h) effectively prevents or blocks HIV infection of monocyte-derived dendritic cells and autologous CD4+ T cells.[2] UC-781 (0.001-1000 µM; 2 h) inhibits viral transfer and infection of cervical explants with HIV-1BaL.[4] |
| In vivo | UC-781（每日一次，连续10天，经阴道给予100 µl 5% UC-781增强凝胶；雌性兔）从凝胶制剂中释放，对雌性兔正常组织显示出低毒性，且不显著增加炎症细胞。[1] |
| Target activity | HIV-1:0.005 μM |
| Synonyms | NSC 675186, UC781, UC 781 |
| molecular weight | 335.85 |
| Molecular formula | C17H18ClNO2S |
| CAS | 178870-32-1 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| References | 1. Balzarini J, et al. Preclinical studies on thiocarboxanilide UC-781 as a virucidal agent. AIDS. 1998;12(10):1129-1138. 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;48(1):337-339. 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;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;79(17):11179-11186. |