Cenicriviroc (TAK-652)

For research use only.

Catalog No.S8512 Synonyms: CVC, TBR-652

1 publication

Cenicriviroc (TAK-652) Chemical Structure

CAS No. 497223-25-3

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.

Selleck's Cenicriviroc (TAK-652) has been cited by 1 publication

Purity & Quality Control

Choose Selective CCR Inhibitors

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 MW\GeY5kfGmxbjDhd5NigQ>? MmTjNUBpeg>? MlPUSIl{eGyjY3Xt[Y51KG:oIGuxNlVKZS2UQV7USXMh\nKxbTDDR3I2KGmwIH3veZNmKE6LSD:zWFMh[2WubIOgZYZ1\XJiMTDodkwhUUN3ME2wMlAxODJ3zszNMi=> MkfvQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2MkW4NVYoRjJ7NEK1PFE3RC:jPh?=
VERO-E6 M3HpcGZ2dmO2aX;uJIF{e2G7 MWi0PEBpenN? MYrUc5hq[2m2eTDDR|UxKGGpYXnud5QhXkWUTz3FOkBk\WyuczDk[ZRmem2rbnXkJIF1KDR6IHjveZJ{KGK7IHjp[4gh[2:wdHXueEBqdWGpaX7nJEh{[W2nIHPvcoRqfGmxboOgZZMhOl:ORWmge4l1cG:3dDDlfJBwe3W{ZTD0c{AxNjBzIF3PTUBUSVKVIFPvWk0zKH[rcoXzLUwhS0N3ME2xNU44O87:TT6= MYK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNVExPzJ5Lze+R4hGVUKOPD;hQi=>

... Click to View More Cell Line Experimental Data

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

Cell Research:

[2]

- Collapse
  • 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.


    (Only for Reference)
Animal Research:

[2]

- Collapse
  • 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
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (143.48 mM)
Water Insoluble
Ethanol '''100 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 696.94
Formula

C41H52N4O4S

CAS No. 497223-25-3
Storage powder
in solvent
Synonyms CVC, TBR-652
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)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation ()
% DMSO % % Tween 80 % ddH2O
CalculateReset

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

  • Mass
    Concentration
    Volume
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and SDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
    V1
    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
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 September 1 2021 Phase 3
NCT05029063 Not yet recruiting Drug: Rivaroxaban 10 MG Venous Thromboembolism|Cancer Ottawa Hospital Research Institute September 2021 Phase 3
NCT04674371 Recruiting Other: central venous catheter insertion Data Collection Wolfram Schummer MD PhD|Deutsche Interdisziplinäre Vereinigung für Intensiv- und Notfallmedizin May 2021 --
NCT04906512 Recruiting Device: Tegaderm CHG Dressing Central Venous Catheter Exit Site Infection|Catheter-Related Infections 3M May 2021 Not Applicable
NCT04767113 Not yet recruiting Drug: Heparin sodium|Drug: Normal saline Cardiac Surgery|Central Venous Catheter Thrombosis|Heparin Guangdong Provincial People''s Hospital March 1 2021 Not Applicable

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

CCR Signaling Pathway Map

Related CCR Products

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
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID