Vicriviroc maleate

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种有效、高选择性、口服生物可利用的 CCR5 拮抗剂，Ki 为 2.5 nM。

A potent, highly selective, and orally bioavailable CCR5 antagonist with Ki of 2.5 nM; display no affinity for muscarinic receptors (Ki>10 uM); inhibits HIV-1 entry into U-80 cells with IC50 of 0.8 nM, inhibits HIV-1 clinical isolates in PBMC with IC90 of 1-10 nM; exhibits excellent receptor selectivity and oral bioavailability in rats and monkeys.HIV Infection Phase 3 Clinical(In Vitro):Vicriviroc maleate (SCH-417690 maleate; SCH-D maleate) is a potent, selective and oral bioavailable inhibitor of CCR5, with a Ki 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.

Vicriviroc maleate (SCH-417690 maleate; SCH-D maleate) is a potent, selective and oral bioavailable inhibitor of CCR5, with a Ki 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.

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.

SCH-417690 | SCH-D

GPCR/G Protein

Chemokine Receptor

CCR5

Infection

HIV Infection

599179-03-0

649.701

C32H42F3N5O6

>98% (HPLC)

10 mM in DMSO

CC1CN(CCN1C(COC)C2=CC=C(C=C2)C(F)(F)F)C3(CCN(CC3)C(=O)C4=C(N=CN=C4C)C)C.C(=CC(=O)O)C(=O)O

Piperidine, 1-[(4,6-dimethyl-5-pyrimidinyl)carbonyl]-4-[(3S)-4-[(1R)-2-methoxy-1-[4-(trifluoromethyl)phenyl]ethyl]-3-methyl-1-piperazinyl]-4-methyl-, (2Z)-2-butenedioate (1:1)

(-20℃)

With Ice Pack

≥ 2 years