| Description | Aplaviroc (AK 602) is a novel and highly potent CCR5 antagonist with antiviral activity that inhibits HIV-1Ba-L, HIV-1JRFL, and HIV-1MOKW and can be used in the study of human immunodeficiency virus infection. |
| In vitro | Aplaviroc 对三种野生型 R5 HIV-1 毒株（HIV-1Ba-L、HIV-1JRFL 和 HIV-1MOKW）的IC50 值为 0.1 至 0.4 nM，并有效阻断 rgp120/sCD4 与CCR5，其 IC50 值为 2.7 nM； Aplaviroc 在极低浓度下（IC50 值为 0.4 至 0.6 nM）抑制两种 HIV-1MDR 变体 HIV-1MM 和 HIV-1JSL 的感染性和复制，由此确定的AplavirocKd值分别为2.9±1.0 nM；Aplaviroc 对抗 R5 HIV-1 的有效活性源于其与 ECL2B 和/或其附近区域的高亲和力结合，从而抑制 gp120/CD4 与 CCR5 的结合 [1]。 |
| In vivo | Apraviroc (AK602) 的浓度在腹腔注射后立即达到最大浓度并迅速下降 [2];Aplaviroc (AK602, 60 mg/kg, bid, daily) 抑制 hu-PBMC-NOG 小鼠中的 R5 HIV-1 病毒血症 [2] 。 |
| Target activity | HIV-1 (MOKW):0.2 nM, HIV-1 (Ba-L):0.4 nM, HIV-1 (JRFL):0.1 nM |
| Synonyms | GSK 873140, ONO-4128, GW 873140, AK 602 |
| molecular weight | 577.71 |
| Molecular formula | C33H43N3O6 |
| CAS | 461443-59-4 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| References | 1. Maeda K, et al. Spirodiketopiperazine-based CCR5 inhibitor which preserves CC-chemokine/CCR5 interactions and exerts potent activity against R5 human immunodeficiency virus type 1 in vitro. J Virol. 2004 Aug;78(16):8654-62. 2. Nakata H, et al. Potent anti-R5 human immunodeficiency virus type 1 effects of a CCR5 antagonist, AK602/ONO4128/GW873140, in a novel human peripheral blood mononuclear cell nonobese diabetic-SCID, interleukin-2 receptor gamma-chain-knocked-out AIDS mouse model. J Virol. 2005 Feb;79(4):2087-96. doi: 10.1128/JVI.79.4.2087-2096.2005. |