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Cenicriviroc Mesylate
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Cenicriviroc Mesylate图片
CAS NO:497223-28-6
包装与价格:
包装价格(元)
25 mg电议
50 mg电议

产品名称
TAK-652 Mesylate
TBR-652 Mesylate
产品介绍

产品描述

Cenicriviroc Mesylate is a dual CCR2/CCR5 antagonist, also inhibits both HIV-1 and HIV-2 with anti-inflammatory and antiinfective activity.

体外活性

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 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 [1]. Phenotypic susceptibility testing shows, for the four R5-tropic HIV-2 isolates, a median EC50 for Cenicriviroc Mesylate of 0.39 nM. The dual-tropic and the X4-tropic HIV-2 strains are resistant to Cenicriviroc Mesylate with EC50 at >1000 nM, and Maximum percentages of inhibition at 33% and 4%, respectively [2].

体内活性

Cenicriviroc Mesylate treatment leads to a dose-related decrease in monocyte/macrophage recruitment and achieving statistical significance at doses ≥20 mg/kg/day. 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) [1].

Cas No.

497223-28-6

分子式

C42H56N4O7S2

分子量

793.05

别名

TAK-652 Mesylate;TBR-652 Mesylate

储存和溶解度

DMSO:100 mg/mL (126.10 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years