599179-03-0
599179-03-0 結(jié)構(gòu)式
基本信息
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-甲基哌啶馬來酸鹽
CS-1868
Unii-ep3qg127N9
SCH-D (maleate)
SCH-417690
SCH-D
VICRIVIROC MALEATE
SCH-417690 (maleate)
vicriviroc Maleate salt
VICRIVIROC MALEATE: SCH-D
Vicriviroc Malate(maleate)
物理化學(xué)性質(zhì)
常見問題列表
|
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.