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Cenicriviroc

Catalog No. TQ0297   CAS 497223-25-3
Synonyms: TAK-652, TBR-652

Cenicriviroc (TAK-652) is an orally active, dual antagonist of CCR2/CCR5. It also inhibits both HIV-1 and HIV-2, and displays potent anti-infective and anti-inflammatory activity.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.
Cenicriviroc Chemical Structure
Cenicriviroc, CAS 497223-25-3
Pack Size Availability Price/USD Quantity
1 mg In stock $ 63.00
2 mg In stock $ 90.00
5 mg In stock $ 129.00
10 mg In stock $ 205.00
25 mg In stock $ 412.00
50 mg In stock $ 532.00
100 mg In stock $ 768.00
200 mg In stock $ 1,080.00
1 mL * 10 mM (in DMSO) In stock $ 221.00
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Purity: 98.98%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Cenicriviroc (TAK-652) is an orally active, dual antagonist of CCR2/CCR5. It also inhibits both HIV-1 and HIV-2, and displays potent anti-infective and anti-inflammatory 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 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. 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 [1].
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].
Synonyms TAK-652, TBR-652
Molecular Weight 696.94
Formula C41H52N4O4S
CAS No. 497223-25-3

Storage

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

Solubility Information

DMSO: 120 mg/mL (172.19 mM)

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. Kuwata T, et al. Incompatible Natures of the HIV-1 Envelope in Resistance to the CCR5 Antagonist Cenicriviroc and to Neutralizing Antibodies. Antimicrob Agents Chemother. 2015 Nov 2;60(1):437-5 3. 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

Related compound libraries

This product is contained In the following compound libraries:
Anti-Fibrosis Compound Library Immunology/Inflammation Compound Library Cytokine Inhibitor Library NO PAINS Compound Library Bioactive Compound Library GPCR Compound Library Clinical Compound Library Immuno-Oncology Compound Library Chemokine Inhibitor Library Human Metabolite Library

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Keywords

Cenicriviroc 497223-25-3 Immunology/Inflammation Microbiology/Virology Proteases/Proteasome HIV Protease CCR CC chemokine receptor TAK-652 inhibit HIV TAK652 Inhibitor Human immunodeficiency virus TAK 652 TBR652 TBR-652 TBR 652 inhibitor

 

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