4-[[1-[3-[(3-クロロ-4-メチルフェニル)(1-アセチル-4-ピペリジニルカルボニル)アミノ]プロピル]-4-ピペリジニル]メチル]ベンズアミド 化學(xué)特性,用途語(yǔ),生産方法
説明
TAK-220 is an orally bioavailable antagonist of chemokine (C-C motif) receptor 5 (CCR5). It binds to CCR5 (IC
50 = 3.5 nM for the human receptor in CHO cells), but not CCR1, CCR2b, CCR3, CCR4, or CCR7. TAK-220 inhibits the binding of chemokine (C-C motif) ligand 5 (CCL5) and CCL3 to CCR5 (IC
50s = 3.5 and 1.4 nM, respectively) but does not inhibit binding of CCL4. It inhibits HIV-1 envelope-mediated membrane fusion in a macrophage (M-tropic) R5, but not in a T cell (T-tropic) X4, strain of HIV-1 (IC
50s = 0.42 and >1,000 nM, respectively). TAK-220 inhibits the replication of six strains of R5 HIV-1 clinical isolates (EC
90 overall mean = 13 nM) and the R5 JR-FL laboratory-adapted strain (EC
50 = 0.6 nM), but not of X4 HIV-1 clinical isolates or the X4 IIIB laboratory-adapted strain (EC
50s = >10,000 nM for both), in human peripheral blood mononuclear cells (PBMCs).
4-[[1-[3-[(3-クロロ-4-メチルフェニル)(1-アセチル-4-ピペリジニルカルボニル)アミノ]プロピル]-4-ピペリジニル]メチル]ベンズアミド 上流と下流の製品情報(bào)
原材料
準(zhǔn)備製品