Vicriviroc (maleate)

Vicriviroc maleate (SCH-417690 maleate; SCH-D maleate) is a potent, selective, oral bioavailable and CNS penetrated antagonist of CCR5, with a K_i of 2.5 nM, and also inhibits HIV-1 in PBMC cells, with IC₉₀s of 3.3 nM (JrFL), 2.8 nM (ADA-M), 1.8 nM (301657), 4.9 nM (JV1083) and 10 nM (RU?570). IC50 & Target: Ki: 2.5 nM (CCR5)^[1]
IC90: 3.3 nM (HIV-1 JrFL, in PBMC cells), 2.8 nM (HIV-1 ADA-M, in PBMC cells), 1.8 nM (HIV-1 301657, in PBMC cells), 4.9 nM (HIV-1 JV1083, in PBMC cells) and 10 nM (HIV-1 RU?570, in PBMC cells)^[1]
In Vitro: 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 IC₉₀s 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 IC₅₀ and IC₉₀ of 0.45 nM and 4 nM for a panel of HIV isolates, and has weak activity against hERG activity (IC₅₀, 5.8 μM)^[1]. Vicriviroc maleate inhibits chemotactic response to MIP-1α with IC₅₀ values below 1 nM, and suppresses RANTES-induced signaling with a mean IC₅₀ of 4.2 ± 1.3 nM. Vicriviroc maleate potently suppresses all the viral isolates tested, with geometric mean EC₅₀s of 0.04-2.3 nM and IC₉₀s of 0.45-18 nM^[2]. In Vivo: 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].