TAK-220 is a selective and orally bioavailable CCR5 antagonist, with IC 50 s of 3.5 nM and 1.4 nM for inhibition on the binding of RANTES and MIP-1α 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 EC 50 s 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 EC 90 s 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.
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