TAK-220

Description

TAK-220 is a selective and orally bioavailable CCR5 antagonist, with IC50s of 3.5 nM and 1.4 nM for inhibition on the binding of RANTES and MIP-1? to CCR5, respectively, but shows no effect on the binding to CCR1, CCR2b, CCR3, CCR4, or CCR7; TAK-220 also selectively inhibits HIV-1, with EC50s of 1.2 nM HIV-1 KK , 0.72 nM HIV-1 CTV , 1.7 nM HIV-1 HKW , 1.7 nM HIV-1 HNK , 0.93 nM HIV-1 HTN , and 0.55 nM HIV-1 HHA , and EC90s of 12 nM HIV-1 KK , 5 nM HIV-1 CTV , 12 nM HIV-1 HKW , 28 nM HIV-1 HNK , 15 nM HIV-1 HTN , and 4 nM HIV-1 HHA in PBMCs.