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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.
| Cell Experiment | |
|---|---|
| Cell lines | activated macrophages |
| Preparation method | 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. |
| Concentrations | 1 μM |
| Incubation time | 2 h |
| Animal Experiment | |
|---|---|
| Animal models | 8-10 weeks old male C57BL/6 mice, 10-12 weeks old male Sprague-Dawley rats |
| Formulation | cenicriviroc mesylate dissolved in 0.5% [w/v] methylcellulose + 1% Tween-80 (pH ~1.3) |
| Dosages | 5 mg/kg, 20 mg/kg, 100 mg/kg, 30 mg/kg |
| Administration | oral gavage (PO) |
| Molecular Weight | 696.94 |
| Formula | C41H52N4O4S |
| CAS Number | 497223-25-3 |
| Solubility (25°C) | DMSO 100 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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