| 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 | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 120 mg/mL (172.18 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 4 mg/mL (5.74 mM), Sonication is recommended.
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| Keywords | TBR652 | TBR 652 | TAK652 | TAK 652 | Inhibitor | inhibit | Human immunodeficiency virus | HIVProtease | HIV-2 | HIV-1 | HIV Protease | HIV | Cenicriviroc | CCR5 | CCR2 | CCR | CC chemokine receptor |
| Inhibitors Related | Stavudine | 5-Fluorouracil | Emtricitabine | Dolutegravir intermediate-1 | Dimethyl fumarate | Lamivudine | Valproic Acid | (-)-Epigallocatechin Gallate | Pirfenidone | Decanedioic acid | Dextran sulfate sodium salt (MW 5000) | Tenofovir |
| Related Compound Libraries | Failed Clinical Trials Compound Library | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Chemokine Inhibitor Library | Anti-Viral Compound Library | Drug Repurposing Compound Library | Inhibitor Library | Anti-Aging Compound Library | Immunology/Inflammation Compound Library | Bioactive Compounds Library Max | GPCR Compound Library | Anti-Infection Compound Library |
United States
