Cas No.: | 599179-03-0 |
Chemical Name: | Vicriviroc maleate |
Synonyms: | Sch 417690,Sch417690 |
SMILES: | N(C(C1=C(C)N=CN=C1C)=O)1CCC(N2CCN([C@@H](C3=CC=C(C(F)(F)F)C=C3)COC)[C@H](C)C2)(C)CC1.C(O)(=O)/C=C/C(O)=O |
Formula: | C32H42F3N5O6 |
M.Wt: | 649.712 |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
Description: | Vicriviroc maleate is a potent, selective, oral bioavailable and CNS penetrated antagonist of CCR5, with a Ki 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). |
In Vivo: | Vicriviroc (10 mg/kg) has good oral availablity in rats and monkeys, with no acute CNS or GI effects in rats[1]. |
In Vitro: | Vicriviroc (Sch-417690/Sch-D) 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 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 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 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]. |