880549-30-4

N-(1H-Benzimidazol-2-ylmethyl)-N-[(8S)-5,6,7,8-tetrahydro-8-quinolinyl]-1,4-butanediamine Monohydrochloride is a potent and selective antagonist of CXCR4. It is also an inhibitor of X4-tropic HIV virus.

AMD070 (AMD11070) is an orally activereversible and selective CXCR4 (CD184fusin) antagonist (IC50 = 13 nM against 100 pM 125I-SDF-1α for binding human CD+/CXCR4+ CEM-CCRF cells) th at inhibits HIV-1 replication in cultures (IC50/host cells = 2 nM/MT-4 and 26 nM/PBMCs; T-tropic HIV-1NL4.3 strain) with no host cytotoxicity even at concentrations above 23 μM.

¹²⁵I-CXCL12-CXCR4: 13 nM (IC₅₀); HIV-1 (NL4.3 strain): 1 nM (IC₅₀, In MT-4 cells); HIV-1 (NL4.3 strain): 9 nM (IC₅₀, In PBMCs); HIV-1 (NL4.3 strain): 3 nM (IC90, In MT-4 cells); HIV-1 (NL4.3 strain): 26 nM (IC90, In PBMCs)