| 產(chǎn)品描述： | Cenicriviroc (CVC, TAK-652, TBR-652) 是一種有效的、口服活性的 CC chemokine receptor 2 (CCR2) 和 CCR5 的雙效抑制劑。Cenicriviroc 還可抑制 HIV-1 和 HIV-2 并具有有效的抗炎和抗感染活性 |
| 靶點(diǎn)： |
CCR2;CCR5;HIV-1;HIV-2;HIVProtease;CCR |
| 體內(nèi)研究： |
Cenicriviroc significantly reduces monocyte/macrophage recruitment in vivo at doses >= 20 mg/kg/day (p < 0.05). At these doses, Cenicriviroc shows antifibrotic effects, with significant reductions in collagen deposition (p < 0.05), and collagen type 1 protein and mRNA expression across the three animal models of fibrosis. In the NASH model, Cenicriviroc significantly reduces the nonalcoholic fatty liver disease activity score (p < 0.05 vs. controls). Cenicriviroc treatment has no notable effect on body or liver/kidney weight. |
| 細(xì)胞實(shí)驗(yàn)： |
Cell lines: activated macrophages Concentrations: 1 μM Incubation Time: 2 h Method: TG is injected intraperitoneally into male C57BL/6 mice and activated macrophages are collected 48 hours later by peritoneal lavage. Chemotaxis is assayed using a Transwell1 Chamber with a 5 μm-pore size polycarbonate filter. Briefly, cells are incubated for 2 hours in the presence of 1 nM CCL2 and/or 1 μM Cenicriviroc (dissolved in dimethyl sulfoxide with 0.5% acetic acid and diluted 1:1000 with serum-free Roswell Park Memorial Institute-1640 medium and 0.5% bovine serum albumin). Cells are harvested from the lower compartment and analyzed by flow cytometry to enumerate F4/80+CD11b+ macrophages using a 3-laser BD FACSCanto. Results are analyzed using FlowJo software. |
| 動(dòng)物實(shí)驗(yàn)： |
Animal Models: 8–10 weeks old male C57BL/6 mice, 10–12 weeks old male Sprague-Dawley rats Dosages: 5 mg/kg, 20 mg/kg, 100 mg/kg, 30 mg/kg Administration: Oral gavage, IP |
| 參考文獻(xiàn)： |
1. Jacob Lalezari, et al. J Acquir Immune Defic Syndr. 2011 Jun 1;57(2):118-25. 2. Eric Lefebvre, et al. PLoS One. 2016 Jun 27;11(6):e0158 |
| 溶解性： |
Soluble in DMSO、Ethanol |
| 保存條件： |
2-8℃ |
| 配置溶液濃度參考： |
|
1mg |
5mg |
10mg |
| 1 mM |
1.435 ml |
7.174 ml |
14.348 ml |
| 5 mM |
0.287 ml |
1.435 ml |
2.87 ml |
| 10 mM |
0.143 ml |
0.717 ml |
1.435 ml |
| 50 mM |
0.029 ml |
0.143 ml |
0.287 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(xiǎn)品化學(xué)品經(jīng)營(yíng)許可證（不帶存儲(chǔ)）
營(yíng)業(yè)執(zhí)照(三證合一)
北京