Cenicriviroc
产品说明书
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同义名 : | TBR-652; TAK-652; CVC |
| CAS号 : | 497223-25-3 | |
| 货号 : | A518613 | |
| 分子式 : | C41H52N4O4S | |
| 纯度 : | 99%+ | |
| 分子量 : | 696.94 | |
| MDL号 : | MFCD28502076 | |
| 存储条件： |
Pure form Sealed in dry, 2-8°C In solvent -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : | - |
| 生物活性 | |||
|---|---|---|---|
| 描述 | Interactions between C-C chemokine receptor types 2 (CCR2) and 5 (CCR5) and their ligands, including C-C chemokine ligand type 2 (CCL2) and CCL5, mediate fibrogenesis by promoting monocyte/macrophage recruitment and tissue infiltration, as well as hepatic stellate cell activation[3]. Cenicriviroc (CVC; also known as TAK-652 and TBR-652) is an orally active, dual CCR2/CCR5 antagonist with IC50 values of 5.9 nM and 0.29 nM in clinical isolates. During the 10-day CVC treatment period, CVC showed a potent dose-response effect on HIV-1 RNA levels which persisted well after discontinuation of treatment. The mean HIV-1 RNA reductions remained significant through day 15 for all CVC dose groups. Those dates suggested CVC to be a potent, well-tolerated anti-HIV drug with potential for additional benefit through a CCR2-mediated anti-inflammatory effect[4]. In the TG-induced model of peritonitis, CVC treatment led to dose-related decreases in monocyte/macrophage recruitment, of similar or greater magnitude than those observed with dexamethasone (positive control), and achieving statistical significance at doses ≥20 mg/kg/day (p < 0.05). In the NASH model, plasma ALT (alanine aminotransferase) levels were significantly decreased with both CVC doses (20 mg/kg/day; 100 mg/kg/day) versus vehicle control (p < 0.05)[3]. | ||
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
1.43mL 0.29mL 0.14mL |
7.17mL 1.43mL 0.72mL |
14.35mL 2.87mL 1.43mL |
| 参考文献 |
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