Cenicriviroc (TAK-652)

Catalog No.S8512 Synonyms: CVC, TBR-652

For research use only.

Cenicriviroc (CVC, TAK-652, TBR-652) 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 (TAK-652) Chemical Structure

CAS No. 497223-25-3

Selleck's Cenicriviroc (TAK-652) has been cited by 2 Publications

Purity & Quality Control

Choose Selective CCR Inhibitors

Other CCR Products

Biological Activity

Description Cenicriviroc (CVC, TAK-652, TBR-652) 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

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 Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
NIH/3T3 NWrCPXJvTnWwY4Tpc44h[XO|YYm= NViy[|lCOSCqch?= M1rKW2Rqe3CuYXPlcYVvfCCxZjDbNVI2UV1vUlHOWGVUKG[{b32gR2NTPSCrbjDtc5V{\SCQSVivN3Q{KGOnbHzzJIFnfGW{IEGgbJItKEmFNUC9NE4xODB{Nd88UU4> NV6zW2ZERGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0NlU5OTZpPkK5OFI2QDF4PD;hQi=>
VERO-E6 MUjGeY5kfGmxbjDhd5NigQ>? NULqXFI4PDhiaILz NV3GR|hrXG:6aXPpeJkhS0N3MDDh[4FqdnO2IG\FVm8uTTZiY3XscJMh\GW2ZYLtbY5m\CCjdDC0PEBpd3W{czDifUBpcWeqIHPvcpRmdnRiaX3h[4lv\yBqc3Ht[UBkd26maYTpc45{KGG|IELfUGV[KHerdHjveZQh\Xiyb4P1doUhfG9iMD6wNUBOV0liU1HSV{BEd1ZvMjD2bZJ2eyluIFPDOVA:OTFwN{ROwG0v NEHPSZA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOTFyN{K3M{c,S2iHTVLMQE9iRg>?
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]

Protocol (from reference)

Cell Research:

[2]

  • 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.

Animal Research:

[2]

  • 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

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 696.94
Formula

C41H52N4O4S

CAS No. 497223-25-3
Storage 3 years -20°C powder
2 years -80°C in solvent
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

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.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT05473299 Not yet recruiting Device: Xeltis Hemodialysis Access (aXess) graft End-stage Renal Disease Xeltis October 31 2022 Not Applicable
NCT05134818 Active not recruiting Other: observer tool Education|Simulation Université Paris-Sud November 2 2021 Not Applicable
NCT05033314 Not yet recruiting Drug: Rivaroxaban 10 MG|Drug: Placebo Sickle Cell Disease|Central Venous Catheter Thrombosis|Venous Thromboembolism Kevin H.M. Kuo MD MSc FRCPC|University Health Network Toronto November 1 2021 Phase 3
NCT05109338 Enrolling by invitation Device: Ben-Guard Garment Central Venous Catheters University of Wisconsin Madison October 1 2021 Not Applicable
NCT05029063 Not yet recruiting Drug: Rivaroxaban 10 MG Venous Thromboembolism|Cancer Ottawa Hospital Research Institute September 2021 Phase 3

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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 (TAK-652) | Cenicriviroc (TAK-652) supplier | purchase Cenicriviroc (TAK-652) | Cenicriviroc (TAK-652) cost | Cenicriviroc (TAK-652) manufacturer | order Cenicriviroc (TAK-652) | Cenicriviroc (TAK-652) distributor