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
BX471 hydrochloride (ZK-811752 hydrochloride) is a potent, selective non-peptide CCR1 antagonist (Ki: 1 nM for human CCR1). It shows 250-fold selectivity for CCR1 over CCR2, CCR5, and CXCR4.
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.