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概述
Cenicriviroc Mesylate (TAK-652 Mesylate) is a dual CCR2/CCR5 antagonist, also inhibits both HIV-1 and HIV-2 , and displays potent anti-inflammatory and antiinfective activity.
In Vitro
Migration of mouse monocytes in response to carbon tetrachloride (CCL2) is reduced following pre-treatment with Cenicriviroc Mesylate (CVC) at a concentration of 1 μM. Compare to untreated and unstimulated cells, the average fold change in migrating cells (±SD) is 0.8±0.2 (p>0.05) and 0.7±0.4 (p>0.05) for CCL2-stimulated cells treated with Cenicriviroc Mesylate and unstimulated cells treated with Cenicriviroc Mesylate, respectively. Phenotypic susceptibility testing shows, for the four R5-tropic HIV-2 isolates, a median EC 50 for Cenicriviroc Mesylate of 0.39 nM (0.03, 0.33, 0.45 and 0.98 nM). The dual-tropic and the X4-tropic HIV-2 strains are resistant to Cenicriviroc Mesylate with EC 50 at >1000 nM, and Maximum percentages of inhibition (MPI) at 33% and 4%, respectively. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Cenicriviroc Mesylate (CVC) treatment leads to dose-related decrease in monocyte/macrophage recruitment, and achieving statistical significance at doses ≥20 mg/kg/day (p<0.05). Compare to the vehicle-control group, peritoneal lavage monocyte/macrophage counts are decreased by: 5.7%, 45.2%, 76.5% and 26.0% for Cenicriviroc Mesylate 5 twice daily (BID), Cenicriviroc Mesylate20 twice daily (BID), Cenicriviroc Mesylate100 BID, Cenicriviroc Mesylate 20 once-daily (QD), respectively. Exposure to Cenicriviroc Mesylate is dose-related and correlated with the decrease in monocyte/macrophage recruitment, with Cenicriviroc Mesylate appearing to be more effective when given BID versus QD, in line with the higher plasma concentrations achieved with BID dosing and the known short half-life in mice (~2 hours) . MCE has not independently confirmed the accuracy of these methods. They are for reference only.
规格
别名
甲磺酸西尼利韦罗
规格或纯度
10mM in DMSO
英文名称
Cenicriviroc Mesylate
生化机理
甲磺酸西尼韦罗（TAK-652 甲磺酸盐）是一种 CCR2/CCR5 双拮抗剂，还能抑制 HIV-1 和 HIV-2，并显示出强大的抗炎和抗感染活性。
储存条件
干燥,-80℃储存
运输条件
特低温运输
作用类型
抑制剂
名称和识别符
EC号
824-584-9
分子类型
小分子
Isomeric SMILES
CCCCOCCOC1=CC=C(C=C1)C2=CC/3=C(C=C2)N(CCC/C(=C3)/C(=O)NC4=CC=C(C=C4)[S@@](=O)CC5=CN=CN5CCC)CC(C)C.CS(=O)(=O)O
PubChem CID
分子量
793.05
高级数据
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| 批号(Lot Number) | 证书类型 | 货号 |
|---|---|---|
 J2622020 |
分析证书 | C654622 |
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