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Vicriviroc maleate

CAS No. : 599179-03-0

MCE 站：Vicriviroc maleate

产品活性：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，K_i 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)。

研究领域：GPCR/G Protein  |  Immunology/Inflammation  |  Anti-infection

作用靶点：CCR  |  HIV

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). 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.

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.

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