CCR5 Inhibitor

DAPTA is a synthetic peptide, functions as a viral entry inhibitor by targeting selectively CCR5, and shows potent anti-HIV activities.

CCX140 (CCX140-B) is a potent CCR2 antagonist.

Nifeviroc is an orally active CCR5 antagonist. Nifeviroc is used for the study of HIV type-1 infection.

CCR5 antagonist 3 (Compound 26) is a CCR5 antagonist with an IC₅₀ of 15.90 nM. CCR5 antagonist 3 shows broad-spectrum anti-HIV-1 activities.

Fuscin, a fungal metabolite, CCR5 receptor antagonist with anti-HIV effects. Fuscin is a respiration and oxidative phosphorylation inhibitor, and also a mitochondrial SH-dependent transport-linked functions inhibitor.

PNU-177864 is a potent, selective, orally active dopamine D₃ receptor antagonist. PNU-177864 induces phospholipid metabolism in vivo and has anti-schizophrenia activity.

HGS004 is a humanized IgG4 monoclonal antibody inhibitor targeting CCR5. HGS004 has potent antivival activity against a diverse panel of CCR5-tropic HIV-1 and durg (such as Maraviroc (HY-13004))-resistant strains. HGS004 can be used for HIV-1 infections research.

CB-0821 is a high affinity CCR5 inhibitor with a K_i of 0.04 nM. CB-0821 binds efficiently to the hydrophobic pocket of the CCR5 protein, to inhibit the interactions between viral protein and CCR5, thereby inhibiting viral entry. CB-0821 has the potential for anti-HIV research.

Ophiobolin C inhibits CCR5 binding to the envelop protein gp120 and CD4, which is responsible for mediating the entry of HIV-1 into cells. Ophiobolin C is also cytotoxic to chronic lymphocytic leukemia cells.