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Cenicriviroc Mesylate

Catalog No. T10756   CAS 497223-28-6
Synonyms: TBR-652 Mesylate, TAK-652 Mesylate

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

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Cenicriviroc Mesylate Chemical Structure
Cenicriviroc Mesylate, CAS 497223-28-6
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Cenicriviroc Mesylate is a dual CCR2/CCR5 antagonist, also inhibits both HIV-1 and HIV-2 with anti-inflammatory and antiinfective activity.
Targets&IC50 CCR5:0.29 nM, CCR2:5.9 nM, R5 HIV-1:0.024-0.08 nM (in PBMCs), R5 HIV-2:0.03-0.98 nM (in PBMCs)
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 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].
In vivo Treatment with Cenicriviroc Mesylate results in a dose-dependent reduction in monocyte/macrophage recruitment, reaching statistical significance at dosages of 20 mg/kg/day or higher. When compared to the vehicle-control group, Cenicriviroc Mesylate administration at dosages of 5 mg twice daily (BID), 20 mg BID, 100 mg BID, and 20 mg once daily (QD) leads to decreases in peritoneal lavage monocyte/macrophage counts of 5.7%, 45.2%, 76.5%, and 26.0%, respectively. The effect of Cenicriviroc Mesylate on reducing monocyte/macrophage recruitment is dose-related and demonstrates a correlation with dosage, showing greater efficacy for twice daily (BID) administration compared to once daily (QD). This increased effectiveness is likely due to the higher plasma concentrations achieved with BID dosing and the compound's short half-life of approximately 2 hours in mice [1].
Synonyms TBR-652 Mesylate, TAK-652 Mesylate
Molecular Weight 793.05
Formula C42H56N4O7S2
CAS No. 497223-28-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 100 mg/mL (126.10 mM), Sonication is recommended.

TargetMolReferences and Literature

1. Lefebvre E, et al. Antifibrotic Effects of the Dual CCR2/CCR5 Antagonist Cenicriviroc in Animal Models of Liver and Kidney Fibrosis. PLoS One. 2016 Jun 27;11(6):e0158156. 2. Visseaux B, et al. Cenicriviroc, a Novel CCR5 (R5) and CCR2 Antagonist, Shows In Vitro Activity against R5 Tropic HIV-2 Clinical Isolates. PLoS One. 2015 Aug 6;10(8):e0134904. 3. Lalezari J, et al. Safety, efficacy, and pharmacokinetics of TBR-652, a CCR5/CCR2 antagonist, in HIV-1-infected, treatment-experienced, CCR5 antagonist-naive subjects. J Acquir Immune Defic Syndr. 2011 Jun 1;57(2):118-25. 4. Baba M, et al. TAK-652 inhibits CCR5-mediated human immunodeficiency virus type 1 infection in vitro and has favorable pharmacokinetics in humans. Antimicrob Agents Chemother. 2005 Nov;49(11):4584-91.

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Keywords

Cenicriviroc Mesylate 497223-28-6 Immunology/Inflammation Microbiology/Virology CCR TBR652 Mesylate TBR-652 Mesylate TAK-652 Mesylate TAK 652 Mesylate TBR 652 Mesylate TAK652 Mesylate inhibitor inhibit

 

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