生物活性
Cenicriviroc, also known as TAK-652 and TBR-652, is an orally active, dual antagonist of CCR2/CCR5. Cenicriviroc inhibits both HIV-1 and HIV-2, and displays potent anti-infective and anti-inflammatory activity. Cenicriviroc (≥20 mg/kg/day) significantly reduces monocyte/macrophage recruitment in vivo. In the NASH model, cenicriviroc significantly reduces the non-alcoholic fatty liver disease activity score. Cenicriviroc treatment has no notable effect on body or liver/kidney weight.
化学数据
| 分子量 | 696.94 |
| 分子式 | C41H52N4O4S |
| CAS号 | 497223-25-3 |
| 纯度 | 99.57% |
| 溶解性（25°C） | DMSO 100 mg/mL |
| 储存和运输条件 | 固体粉末： -20°C 冷藏长期储存
常温运输及临时存放 |
实验操作 来自于公开的文献，仅供相同实验参考（如实验材料、目的不同，请参考其他文献）
| 细胞实验 |
|---|
| 细胞系 | activated macrophages |
| 方法 | 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. |
| 浓度 | 1 μM |
| 处理时间 | 2 h |
| 动物实验 |
|---|
| 动物模型 | 8-10 weeks old male C57BL/6 mice, 10-12 weeks old male Sprague-Dawley rats |
| 配制 | cenicriviroc mesylate dissolved in 0.5% [w/v] methylcellulose + 1% Tween-80 (pH ~1.3) |
| 剂量 | 5 mg/kg, 20 mg/kg, 100 mg/kg, 30 mg/kg |
| 给药处理 | oral gavage (PO) |
不同实验动物依据体表面积的等效剂量转换表（数据来源于FDA指南）
| 小鼠 | 大鼠 | 兔 | 豚鼠 | 仓鼠 | 狗 |
| 重量 (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| 体表面积 (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km系数 | 3 | 6 | 12 | 8 | 5 | 20 |
| 动物 A (mg/kg) = 动物 B (mg/kg) × | 动物 B的Km系数 |
| 动物 A的Km系数 |
例如，依据体表面积折算法，将化合物用于小鼠的剂量20 mg/kg 换算成大鼠的剂量，需要将20 mg/kg 乘以小鼠的Km系数（3），再除以大鼠的Km系数（6），得到化合物用于大鼠的等效剂量为10 mg/kg。
储备液配制
以下数据基于产品分子量，对于特殊产品，请参照COA中的储备液配制条件和说明进行操作。
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 1.4348 mL | 7.1742 mL | 14.3484 mL |
| 5 mM | 0.287 mL | 1.4348 mL | 2.8697 mL |
| 10 mM | 0.1435 mL | 0.7174 mL | 1.4348 mL |
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