Home Immunology & Inflammation CCR inhibitor - HIV inhibitor Cenicriviroc For research use only.

Cenicriviroc

Synonyms: TAK-652, CVC, TBR-652

Cenicriviroc is a potent, orally active dual inhibitor of CC chemokine receptor 2 (CCR2) and CCR5. Cenicriviroc also inhibits HIV-1 and HIV-2 with potent anti-inflammatory and antiinfective activity.

Cenicriviroc Chemical Structure

Cenicriviroc Chemical Structure

CAS No. 497223-25-3

Purity & Quality Control

Cenicriviroc Related Products

Signaling Pathway

CCR Signaling Pathways

CCR Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
NIH/3T3 Function assay 1 hr Displacement of [125I]-RANTES from CCR5 in mouse NIH/3T3 cells after 1 hr, IC50=0.00025μM. 29425816
VERO-E6 Function assay 48 hrs Toxicity CC50 against VERO-E6 cells determined at 48 hours by high content imaging (same conditions as 2_LEY without exposure to 0.01 MOI SARS CoV-2 virus), CC50=11.73μM. ChEMBL
Click to View More Cell Line Experimental Data

Biological Activity

Description Cenicriviroc is a potent, orally active dual inhibitor of CC chemokine receptor 2 (CCR2) and CCR5. Cenicriviroc also inhibits HIV-1 and HIV-2 with potent anti-inflammatory and antiinfective activity.
Targets
CCR2 [1] CCR5 [1] HIV-1 [1] HIV-2 [1]
In vitro
In vitro

Migration of mouse monocytes in response to CCL2, the most potent mediator of chemotaxis for activated macrophages, is reduced following pre-treatment with Cenicriviroc at a concentration of 1 μM.[2]
Cell Research Cell lines activated macrophages
Concentrations 1 μM
Incubation Time 2 h
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.
In Vivo
In vivo

Cenicriviroc significantly reduces monocyte/macrophage recruitment in vivo at doses >= 20 mg/kg/day (p < 0.05). At these doses, Cenicriviroc shows antifibrotic effects, with significant reductions in collagen deposition (p < 0.05), and collagen type 1 protein and mRNA expression across the three animal models of fibrosis. In the NASH model, Cenicriviroc significantly reduces the nonalcoholic fatty liver disease activity score (p < 0.05 vs. controls). Cenicriviroc treatment has no notable effect on body or liver/kidney weight.[2]
Animal Research Animal Models 8–10 weeks old male C57BL/6 mice, 10–12 weeks old male Sprague-Dawley rats
Dosages 5 mg/kg, 20 mg/kg, 100 mg/kg, 30 mg/kg
Administration Oral gavage, IP
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06329310 Not yet recruiting
End Stage Renal Disease
Xeltis
 July 2024 Not Applicable
NCT06190717 Recruiting
Diabetes|End Stage Renal Disease
Sonavex Inc.
 February 21 2024 Not Applicable
NCT06310174 Recruiting
Central Venous Catheter Exit Site Infection
Johns Hopkins University
 December 22 2023 --
NCT06121115 Completed
Septic Shock|Hypotension and Shock
Region Skane
 October 3 2023 --
NCT05896735 Recruiting
Multiple Trauma/Injuries
Second Affiliated Hospital School of Medicine Zhejiang University
 April 25 2023 --
NCT05751395 Not yet recruiting
Central Venous Catheter
Deutsche Interdisziplinäre Vereinigung für Intensiv- und Notfallmedizin
 March 1 2023 --

Chemical Information & Solubility

Molecular Weight 696.94 Formula

C41H52N4O4S
CAS No. 497223-25-3 SDF --
Smiles CCCCOCCOC1=CC=C(C=C1)C2=CC3=C(C=C2)N(CCCC(=C3)C(=O)NC4=CC=C(C=C4)S(=O)CC5=CN=CN5CCC)CC(C)C
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 100 mg/mL ( (143.48 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 100 mg/mL

Water : Insoluble


Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

Preparing Stock Solutions

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

* Indicates a Required Field

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.
Tags: buy Cenicriviroc | Cenicriviroc supplier | purchase Cenicriviroc | Cenicriviroc cost | Cenicriviroc manufacturer | order Cenicriviroc | Cenicriviroc distributor