Cenicriviroc

Description: Cenicriviroc (formerly known as TAK-652 or TBR-652) is a novel, orally bioactive, and dual antagonist of CCR2/CCR5, it also inhibits both HIV-1 and HIV-2, and has the potential for the treatment of HIV infection. TAK-652 inhibited the binding of RANTES (regulated on activation, normal T-cell expressed and secreted), macrophage inflammatory protein 1alpha (MIP-1alpha), and MIP-1beta to CCR5-expressing cells at nanomolar concentrations. TAK-652 could also suppress the binding of monocyte chemotactic protein 1 (MCP-1) to CCR2b-expressing cells. However, its inhibitory effect on ligand binding to other chemokine receptors was limited. TAK-652 was active against CCR5-using (R5) HIV-1 but totally inactive against CXCR4-using (X4) HIV-1.

References: Antimicrob Agents Chemother. 2005 Nov; 49(11):4584-91; PLoS One. 2015 Aug 6; 10(8):e0134904.

Related CAS# 497223-25-3 (free base); 497223-28-6 (mesylate);