Molecular Formula | C32H42F3N5O6 |
Molar Mass | 649.7009896 |
Boling Point | 608.1°C at 760 mmHg |
Flash Point | 321.5°C |
Vapor Presure | 9.89E-15mmHg at 25°C |
Storage Condition | 2-8℃ |
In vitro study | 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. |
In vivo study | 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. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 1.539 ml | 7.696 ml | 15.392 ml |
5 mM | 0.308 ml | 1.539 ml | 3.078 ml |
10 mM | 0.154 ml | 0.77 ml | 1.539 ml |
5 mM | 0.031 ml | 0.154 ml | 0.308 ml |
biological activity | Vicriviroc maleate (SCH-417690 maleate; SCH-D maleate) is an effective, selective, A CCR5 antagonist that can cross the blood-brain barrier with a Ki of 2.5 nM and a HIV-1 inhibition of activity in peripheral blood mononuclear cells with an IC90 of 3.3 nM (JrFL),2.8 nM (ADA-M),1.8 nM (301657),4.9 nM (JV1083) and 10 nM (RU 570). |