| Name | Cenicriviroc |
| Description | Cenicriviroc (TAK-652) is an orally active, dual CCR2/CCR5 antagonist that inhibits both HIV-1 and HIV-2, exhibiting potent anti-infective and anti-inflammatory activity. |
| Animal Research | Male C57BL/6 mice (n=44; 8-10 weeks of age) are allocated to receive treatments via oral gavage (PO) on Days 1-5 in the following groups: non-disease control, vehicle control twice daily (BID), Cenicriviroc 5 mg/kg/day (Cenicriviroc5) BID, Cenicriviroc 20 mg/kg/day (Cenicriviroc20) BID, Cenicriviroc 100 mg/kg/day (Cenicriviroc100) BID, Cenicriviroc20 QD, and positive control (corticosteroid known to reduce inflammation in a variety of animal models) 1 mg/kg QD. On Day 4, peritonitis is induced via IP injection of TG 3.85% (1 mL/animal) 2 hours post-dose in all groups except non-disease controls [1]. |
| In vitro | Cenicriviroc prevents HIV-1 from cellular entry [2]. Regarding the 4 R5 HIV-2 clinical isolates tested, effective concentration 50% EC50 for cenicriviroc are 0.03, 0.33, 0.45 and 0.98 nM. The dual-tropic and the X4-tropic HIV-2 strains are resistant to cenicriviroc with EC50 at >1000 nM, and MPI at 33% and 4%, respectively [3]. |
| In vivo | Cenicriviroc (≥20 mg/kg/day) significantly reduces monocyte/macrophage recruitment in vivo and lowers the non-alcoholic fatty liver disease activity score in the NASH model, without affecting body, liver, or kidney weight [1]. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 120 mg/mL (172.19 mM)
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| Keywords | CC chemokine receptor | Cenicriviroc | inhibit | HIV | TAK652 | Inhibitor | Human immunodeficiency virus | TAK 652 | TBR652 | TBR 652 | CCR |
| Inhibitors Related | Stavudine | 5-Fluorouracil | Inosine pranobex | Emtricitabine | Kaempferol | Dolutegravir intermediate-1 | Dextran sulfate sodium salt (MW 4500-5500) | Lamivudine | Chloroquine phosphate | Decanedioic acid | Pirfenidone | Tenofovir |
| Related Compound Libraries | Bioactive Compound Library | Cytokine Inhibitor Library | Membrane Protein-targeted Compound Library | ReFRAME Related Library | Drug Repurposing Compound Library | Anti-Viral Compound Library | Inhibitor Library | Immuno-Oncology Compound Library | Anti-Aging Compound Library | Bioactive Compounds Library Max |
United States
