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TAK-779 is a potent and selective nonpeptide antagonist of CCR5 and CXCR3, with a Ki of 1.1 nM for CCR5, and effectively and selectively inhibits R5 HIV-1, with EC50 and EC90 of 1.2 nM and 5.7 nM, respectively, in MAGI-CCR5 cells. MIP-1α-CCR5|1 nM (IC50, in CHO/CCR5 cells)|MIP-1β-CCR5|1 nM (IC50, in CHO/CCR5 cells)|RANTES-CCR5|1.4 nM (IC50, in CHO/CCR5 cells)|MCP-1-CCR2b|27 nM (IC50, in CHO/CCR5 cells)|R5 HIV-1 (Ba-L)|1.2 nM (EC50, in MAGI-CCR5 cells)|R5 HIV-1 (KK)|1.6 nM (EC50, in PBMCs)|R5 HIV-1 (HHA)|3.2 nM (EC50, in PBMCs)|R5 HIV-1 (CTV)|3.5 nM (EC50, in PBMCs)|R5 HIV-1 (Ba-L)|3.7 nM (EC50, in PBMCs)|R5 HIV-1 (Ba-L)|5.7 nM (EC90, in MAGI-CCR5 cells)|R5 HIV-1 (HHA)|7.5 nM (EC90, in PBMCs)|R5 HIV-1 (Ba-L)|12.8 nM (EC90, in PBMCs)|R5 HIV-1 (KK)|20.8 nM (EC90, in PBMCs)|R5 HIV-1 (CTV)|27 nM (EC90, in PBMCs)|mCXCR3|369 nM (IC50, in PBMCs)

TAK-779 is a potent and selective nonpeptide antagonist of CCR5, with a Ki of 1.1 nM, and effectively and selectively inhibits R5 HIV-1, with EC50 and EC90 of 1.2 nM and 5.7 nM, respectively, in MAGI-CCR5 cells. TAK-779 less potently blocks the binding of [125I]-monocyte chemotactic protein 1 to CCR2b in CHO/CCR2b cells, with an IC50 for CCR2b of 27 nM. TAK-779 also completely inhibits the binding of [125I]-RANTES to CHO/CCR5 cells with an IC50 of 1.4 nM. TAK-779 (20 nM) selectively inhibits CCR5-mediated Ca2+-signaling. In addition, TAK-779 shows no inhibition on X4 HIV-1 strains[1]. TAK-779 is an antagonist of CXCR3, and inhibits the migration of T cells but not T cell proliferation[2].

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