| Name | Aplaviroc |
| Description | Aplaviroc (AK 602), an SDP derivative, is a CCR5 antagonist with IC50 values of 0.1-0.4 nM for HIV-1Ba-L, HIV-1JRFL, and HIV-1MOKW. |
| In vitro | Aplaviroc showed an IC50 value of 0.1 to 0.4 nM for the three wild-type R5 HIV-1 strains (HIV-1Ba-L, HIV-1JRFL, and HIV-1MOKW) and effectively blocked rgp120/sCD4 and CCR5 with an IC50 value of 2.7 nM; Aplaviroc inhibited the infectivity and replication of the two HIV-1MDR variants, HIV-1MM and HIV-1JSL, at very low concentrations (IC50 value 0.4 to 0.6 nM), while the two R5 HIV-1 variants inhibited zidovudine, nelfinavir, and nafenacil. Aplaviroc inhibits the infectivity and replication of the two HIV-1MDR variants, HIV-1MM and HIV-1JSL, at very low concentrations (IC50 values of 0.4 to 0.6 nM), resulting in AplavirocKd values of 2.9±1.0 nM, respectively; Aplaviroc's potent activity against R5 HIV-1 stems from its high-affinity binding to ECL2B and/or its neighboring regions, which leads to inhibition of the interaction between rgp120/CD4 and CCR5. gp120/CD4 binding to CCR5 [1]. |
| In vivo | The concentration of apraviroc (AK602) reaches maximum concentration immediately after intraperitoneal administration and decreases rapidly [2];Aplaviroc (AK602, 60 mg/kg, bid, daily) inhibits R5 HIV-1 viremia in hu-PBMC-NOG mice[2]. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
| Keywords | HIVProtease | HIV-1MOKW | HIV-1JRFL | HIV-1Ba-L | HIV Protease | HIV | GW-873140 | GW873140 | GSK-873140 | GSK873140 | CCR5 | Aplaviroc | AK-602 | AK602 |
| Inhibitors Related | Stavudine | 5-Fluorouracil | Emtricitabine | Kaempferol | Dolutegravir intermediate-1 | Dimethyl fumarate | Lamivudine | Chloroquine phosphate | Valproic Acid | Decanedioic acid | Dextran sulfate sodium salt (MW 5000) | Tenofovir |
| Related Compound Libraries | Bioactive Compound Library | Cytokine Inhibitor Library | Chemokine Inhibitor Library | Drug Repurposing Compound Library | Inhibitor Library | Immuno-Oncology Compound Library | Immunology/Inflammation Compound Library | Bioactive Compounds Library Max | GPCR Compound Library | Anti-Infection Compound Library | Human Metabolite Library |
United States
