| 產(chǎn)品描述： | Vicriviroc maleate (SCH-417690 maleate; SCH-D 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). |
| 靶點： |
CCR5:2.5 nM (Ki);CCR5;HIV-1;HIV-1 (301657):1.8 nM (IC90, in PBMC cells);HIV-1 (ADA-M):2.8 nM (IC90, in PBMC cells);HIV-1 (JrFL):3.3 nM (IC90, in PBMC cells);HIV-1 (JV1083):4.9 nM (IC90, in PBMC cells);HIV-1 (RU 570):10 nM (IC90, in PBMC cells);HIVProtease;CCR |
| 體內(nèi)研究： |
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 |
| 參考文獻(xiàn)： |
1. Tagat JR, et al. Piperazine-based CCR5 antagonists as HIV-1 inhibitors. IV. Discovery of 1-[(4,6-dimethyl-5-pyrimidinyl)carbonyl]- 4-[4-[2-methoxy-1(R)-4-(trifluoromethyl)phenyl]ethyl-3(S)-methyl-1-piperazinyl]- 4-methylpiperidine (Sch-417690/Sch-D), a potent, highly selective, and orally bioavailable CCR5 antagonist. J Med Chem. 2004 May 6;47(10):2405-8. 2. Strizki JM, et al. Discovery and characterization of vicriviroc (SCH 417690), a CCR5 antagonist with potent activity against human immunodeficiency virus type 1. Antimicrob Agents Chemother. 2005 Dec;49(12):4911-9. |
| 溶解性： |
Soluble in DMSO、H2O |
| 保存條件： |
2-8℃ |
| 配置溶液濃度參考： |
|
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 |
| 50 mM |
0.031 ml |
0.154 ml |
0.308 ml |
|
| 注意： |
部分產(chǎn)品我司僅能提供部分信息，我司不保證所提供信息的權(quán)威性，僅供客戶參考交流研究之用。 |
上海工商
危險品化學(xué)品經(jīng)營許可證（不帶存儲）
營業(yè)執(zhí)照(三證合一)
北京