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Cenicriviroc

Cat. No. M10190
Cenicriviroc Structure
Synonym:

TAK-652; TBR-652

Size Price Availability Quantity
5mg USD 220  USD220 In stock
10mg USD 380  USD380 In stock
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Quality Control & Documentation
Biological Activity

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.

Protocol (for reference only)
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)
Chemical Information
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
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Feng Liang, et al. PLoS One. The dual CCR2/CCR5 chemokine receptor antagonist Cenicriviroc reduces macrophage infiltration and disease severity in Duchenne muscular dystrophy (Dmdmdx-4Cv) mice

[2] Eric Lefebvre, et al. PLoS One. Antifibrotic Effects of the Dual CCR2/CCR5 Antagonist Cenicriviroc in Animal Models of Liver and Kidney Fibrosis

[3] Takeo Kuwata, et al. Antimicrob Agents Chemother. Incompatible Natures of the HIV-1 Envelope in Resistance to the CCR5 Antagonist Cenicriviroc and to Neutralizing Antibodies

[4] Jacob Lalezari, et al. J Acquir Immune Defic Syndr. Safety, efficacy, and pharmacokinetics of TBR-652, a CCR5/CCR2 antagonist, in HIV-1-infected, treatment-experienced, CCR5 antagonist-naive subjects

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Keywords: Cenicriviroc, TAK-652; TBR-652 supplier, CCR, inhibitors, activators


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