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• 产品描述：

  Cenicriviroc (CVC, TAK-652, TBR-652) 是一种有效的、口服活性的 CC chemokine receptor 2 (CCR2) 和 CCR5 的双效抑制剂。Cenicriviroc 还可抑制 HIV-1 和 HIV-2 并具有有效的抗炎和抗感染活性

• 靶点： CCR2;CCR5;HIV-1;HIV-2;HIVProtease;CCR

• 体内研究：
  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.

• 细胞实验： 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.

• 动物实验： 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

• 参考文献：
  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

• 保存条件： 2-8℃

• 配置溶液浓度参考：
  

  	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

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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *