AMD 3465 also potently inhibits the replication of X4 HIV strains (IC50: 1-10 nM). However, it has no effect on CCR5-using (R5) viruses. AMD 3465 (GENZ-644494) is a potent antagonist of CXCR4, inhibits binding of 12G5 mAb and CXCL12AF647 to CXCR4, with IC
Gnidimacrin activated HIV-1 replication and killed persistently-infected cells at picomolar concentrations. In addition to its potential to purge HIV-1 from latently infected cells, gnidimacrin potently inhibited a panel of HIV-1 R5 virus infection of peripheral blood mononuclear cells (PBMCs) at an average concentration lower than 10 pM. These results suggest that gnidimacrin could activate latent HIV-1, specifically kill HIV-1 persistently infected cells, and inhibit R5 viruses at picomolar concentrations
AMD-3451 free base is a dual CCR5 CXCR4 antagonist which may be useful in the treatment of a wide variety of R5, R5 X4, and X4 strains of human immunodeficiency virus type 1 (HIV-1) and HIV-2. AMD3451 is the first low-molecular-weight anti-HIV agent with selective HIV coreceptor, CCR5 and CXCR4, interaction.