| Bioactivity | 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]. |
| Invitro | UC-781 (0.05、0.2 和 0.5 % UC-781 补充凝胶；10 d) 从凝胶制剂中释放出来，并清除 CEM 细胞中的 HIV-1[1]。UC-781 (3.75 -30 μM) 抑制蜡样芽孢杆菌的生长 (约 50 %)[1]。UC-781 抑制 CEM T 细胞中的 HIV-1 (ⅢB) 活性 (EC50=6 nM; IC50=23 nM)。UC-781 抑制单核细胞来源的树突状细胞 (MO-DC) 和自体 CD4+ T 细胞中的 HIV 活性，EC50 值分别为 550 nM 和 1588 nM[2]。UC-781 (1000 nM；24 h) 有效地防止或阻止了单核细胞来源的树突状细胞和自体 CD4+ T 细胞感染 HIV[2]。UC-781 (0.001-1000 µM；2 h) 抑制病毒转移和宫颈外植体感染 HIV-1BaL[4]。 |
| In Vivo | UC-781 (100 µl 5% UC-781 补充凝胶；阴道内；一天一次持续 10 天) 从凝胶制剂中释放出来，对雌兔正常组织显示低毒性[1]。 Animal Model: |
| Name | UC-781 |
| CAS | 178870-32-1 |
| Formula | C17H18ClNO2S |
| Molar Mass | 335.85 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [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. |