Highly potent CXCR4 antagonist; inhibits HIV-1 replication
Highly potent CXCR4 antagonist (IC50 = 0.61 nM). Displays selectivity for CXCR4 over a range of other CXC receptors. Inhibits replication of HIV-1 viruses in human PBMC (EC50 values are 0.33 to 1.4 nM). Supresses HIV-1 infection in mice. Orally bioavailable.
Murakami et al (2009) The novel CXCR4 antagonist KRH-3955 is an orally bioavailable and extremely potent inhibitor of human immunodeficiency virus type 1 infection: comparative studies with AMD3100. Antimicrob.Agents Chemother. 53 2940 PMID:19451305 |Iwasaki et al (2009) Efficient inhibition of SDF-1α-mediated chemotaxis and HIV-1 infection by novel CXCR4 antagonists. Cancer Sci. 100 778 PMID:19245436
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