1-[(4,6-二甲基-5-嘧啶基)羰基]-4-[(3S)-4-[(1R)-2-甲氧基-1-[4-(三氟甲基)苯基]乙基]-3-甲基-1-哌嗪基]-4-甲基哌啶马来酸盐性质、用途与生产工艺
Vicriviroc maleate (SCH-417690 maleate; SCH-D maleate) 是一种有效，选择性，可口服，可透过血脑屏障的 CCR5 拮抗剂，Ki 值为 2.5 nM，同时抑制外周血单核细胞中的 HIV-1 的活性，IC90 值分别为 3.3 nM (JrFL)，2.8 nM (ADA-M)，1.8 nM (301657)，4.9 nM (JV1083) 和 10 nM (RU 570)。
|
CCR5
2.5 nM (Ki)
|
HIV-1 (JrFL)
3.3 nM (IC90, in PBMC cells)
|
HIV-1 (ADA-M)
2.8 nM (IC90, in PBMC cells)
|
HIV-1 (301657)
1.8 nM (IC90, in PBMC cells)
|
HIV-1 (JV1083)
4.9 nM (IC90, in PBMC cells)
|
HIV-1 (RU 570)
10 nM (IC90, in PBMC cells)
|
Vicriviroc maleate (SCH-417690 maleate; SCH-D maleate) is a potent, selective and oral bioavailable inhibitor of CCR5, with a K
i
of 2.5 nM, and also inhibits HIV-1 in PBMC cells, with IC
90
s of 3.3 (JrFL), 2.8 (ADA-M), 1.8 (301657), 4.9 (JV1083) and 10 nM (RU 570). In addition, Vicriviroc maleate shows a mean IC
50
and IC
90
of 0.45 nM and 4 nM for a panel of HIV isolates, and has weak activity against hERG activity (IC
50
, 5.8 μM). Vicriviroc maleate inhibits chemotactic response to MIP-1α with IC
50
values below 1 nM, and suppresses RANTES-induced signaling with a mean IC
50
of 4.2 ± 1.3 nM. Vicriviroc maleate potently suppresses all the viral isolates tested, with geometric mean EC
50
s of 0.04-2.3 nM and IC
90
s of 0.45-18 nM.
Vicriviroc maleate (SCH-417690 maleate; SCH-D maleate; 10 mg/kg) has good oral availablity in rats and monkeys, with no acute CNS or GI effects in rats.
1-[(4,6-二甲基-5-嘧啶基)羰基]-4-[(3S)-4-[(1R)-2-甲氧基-1-[4-(三氟甲基)苯基]乙基]-3-甲基-1-哌嗪基]-4-甲基哌啶马来酸盐
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