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

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.