2. GPCR/G Protein Immunology/Inflammation Anti-infection
  3. CCR HIV
  4. Cenicriviroc Mesylate

Cenicriviroc Mesylate  (Synonyms: TAK-652 Mesylate; TBR-652 Mesylate)

Cat. No.: HY-14882A Purity: 99.94%
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Cenicriviroc Mesylate (TAK-652 Mesylate) is a dual CCR2/CCR5 antagonist, also inhibits both HIV-1 and HIV-2, and displays potent anti-inflammatory and antiinfective activity.

For research use only. We do not sell to patients.

CAS No. : 497223-28-6

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Solution
10 mM * 1 mL in DMSO In-stock
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Customer Review

Based on 7 publication(s) in Google Scholar

Other Forms of Cenicriviroc Mesylate:

Cenicriviroc Mesylate Related Antibodies

Top Publications Citing Use of Products

    Cenicriviroc Mesylate purchased from MedChemExpress. Usage Cited in: Am J Physiol Cell Physiol. 2024 Feb 1;326(2):C487-C504.  [Abstract]

    Evaluation of CVC (Cenicriviroc) (24 h) antiviral activity against different HIV-1 strains in primary human astrocytes. Cells were infected with HIV-1 NL4-3, YU-2, and JR-CSF in the presence of CVC (1 μM) or vehicle (0.1% DMSO). Cell cultures were washed after 12 h of infection and resuspended in 1 mL of fresh medium containing CVC or vehicle to maintain constant drug/vehicle levels for the duration of the experiment. HIV-1 p24 levels in the supernatants were determined at the indicated time points. Note that CVC effectively protected against astrocyte infection by the JR-CSF strain.

    Cenicriviroc Mesylate purchased from MedChemExpress. Usage Cited in: Am J Physiol Cell Physiol. 2024 Feb 1;326(2):C487-C504.  [Abstract]

    Effect of CVC (Cenicriviroc) (1 μM; 24 h) on endothelial permeability after OGD/R exposure and HIV-1 infection of astrocytes. Permeability was assessed by adding 10 kDa fluorescein isothiocyanate (FITC)-dextran (0.1 mg/mL) to the upper compartment of the Transwell system, followed by spectrophotometric measurement of its passage through human brain microvascular endothelial cell (HBMEC) monolayers into the lower compartment for 1 h.

    Cenicriviroc Mesylate purchased from MedChemExpress. Usage Cited in: Am J Physiol Cell Physiol. 2024 Feb 1;326(2):C487-C504.  [Abstract]

    Cenicriviroc (CVC) (1 μM; 24 h). Representative images of Western blots for the tight junction (TJ) proteins zona occludens 1 (ZO-1), occludin, and claudin-5.

    Cenicriviroc Mesylate purchased from MedChemExpress. Usage Cited in: Am J Physiol Cell Physiol. 2024 Feb 1;326(2):C487-C504.  [Abstract]

    Representative confocal immunofluorescence staining images of NLRP3 (green), ASC (red), and nuclei (blue). Scale bar: 50 μm.The results showed that the colocalization of NLRP3 with ASC was increased in OGD/R-treated infected astrocytes compared with the control, and this effect was partially alleviated by CVC (Cenicriviroc) (1 μM; 24 h) treatment, which suggests reduced inflammasome formation and activation.

    Cenicriviroc Mesylate purchased from MedChemExpress. Usage Cited in: Biomaterials. 2021 Jan;265:120392.  [Abstract]

    The toxicity experiment of CCR5 inhibitor (Cenicriviroc) in zebrafish. Represent imaging of Tg (mpx:EGFP) larvae were treated with control buffer and 5 µM, 10 µM, 20 µM CCR5 inhibitor (Cenicriviroc) (24 h). Scale bar: 500 µm. The MPX+ cells number of whole body in Tg (mpx:EGFP) larvae.

    Cenicriviroc Mesylate purchased from MedChemExpress. Usage Cited in: Biomaterials. 2021 Jan;265:120392.  [Abstract]

    Represented imaging of macrophages recruitment to wounds in 72 hpf Tg (mpx:EGFP) larvae treated with control buffer and CCR5 inhibitor (Cenicriviroc) (5-20 µM; 24 h) with Imaris analysis. Scale bar: 200 μm.

    Cenicriviroc Mesylate purchased from MedChemExpress. Usage Cited in: Cells. 2020 Apr 14;9(4):964.  [Abstract]

    These spheroids were repeatedly exposed to different anti-NASH drugs, from day 7 to 14, with renewed drug exposure every alternate day. Expression of COL1A1 protein was reduced for Cenicriviroc (3 μM; continuous supplementation in culture medium; medium was refreshed every other day during day 7–14), elafibranor, and lanifibranor.

    View All CCR Isoform Specific Products:

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    CCR1 CCR2 CCR3 CCR4 CCR5 CCR6 CCR7 CCR8 CCR9

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    HIV HIV-1 HIV-2

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Cenicriviroc Mesylate (TAK-652 Mesylate) is a dual CCR2/CCR5 antagonist, also inhibits both HIV-1 and HIV-2, and displays potent anti-inflammatory and antiinfective activity.

    IC50 & Target[2][3][4]

    CCR5

    0.29 nM (IC50)

    CCR2

    5.9 nM (IC50)

    R5 HIV-1

    0.024-0.08 nM (IC50, in PBMCs)

    R5 HIV-2

    0.03-0.98 nM (IC50, in PBMCs)

    Cellular Effect
    Cell Line Type Value Description References
    CHO IC50
    >10000 nM
    Compound: (S)-(-)-5b
    Displacement of [125I]RANTES from CCR1 expressed in CHO cells
    Displacement of [125I]RANTES from CCR1 expressed in CHO cells
    		[PMID: 16539392]
    CHO IC50
    1100 nM
    Compound: (S)-(-)-5b
    Displacement of [125I]TARC from CCR4 expressed in CHO cells
    Displacement of [125I]TARC from CCR4 expressed in CHO cells
    		[PMID: 16539392]
    CHO IC50
    2400 nM
    Compound: (S)-(-)-5b
    Displacement of [125I]eotaxin from CCR3 expressed in CHO cells
    Displacement of [125I]eotaxin from CCR3 expressed in CHO cells
    		[PMID: 16539392]
    CHO IC50
    3.1 nM
    Compound: (S)-(-)-5b
    Displacement of [125I]RANTES from CCR5 expressed in CHO cells
    Displacement of [125I]RANTES from CCR5 expressed in CHO cells
    		[PMID: 16539392]
    CHO IC50
    5.9 nM
    Compound: (S)-(-)-5b
    Displacement of [125I]MCP-1 from CCR2b expressed in CHO cells
    Displacement of [125I]MCP-1 from CCR2b expressed in CHO cells
    		[PMID: 16539392]
    CHO IC50
    >10000 nM
    Compound: (S)-(-)-5b
    Displacement of [125I]MIP-3beta from CCR7 expressed in CHO cells
    Displacement of [125I]MIP-3beta from CCR7 expressed in CHO cells
    		[PMID: 16539392]
    COS-7 IC50
    0.1 nM
    Compound: (S)-(-)-5b
    Inhibition of membrane fusion between HIV1 JR-FL Env-expressing COS7 cells and MOLT4/CCR5
    Inhibition of membrane fusion between HIV1 JR-FL Env-expressing COS7 cells and MOLT4/CCR5
    		[PMID: 16539392]
    MOLT-4 IC50
    0.2 nM
    Compound: (S)-(-)-5b
    Inhibition of replication of R5 HIV1 Ba-L in MOLT4/CCR5 cells
    Inhibition of replication of R5 HIV1 Ba-L in MOLT4/CCR5 cells
    		[PMID: 16539392]
    In Vitro

    Migration of mouse monocytes in response to carbon tetrachloride (CCL2) is reduced following pre-treatment with Cenicriviroc Mesylate (CVC) at a concentration of 1 μM. Compare to untreated and unstimulated cells, the average fold change in migrating cells (±SD) is 0.8±0.2 (p>0.05) and 0.7±0.4 (p>0.05) for CCL2-stimulated cells treated with Cenicriviroc Mesylate and unstimulated cells treated with Cenicriviroc Mesylate, respectively[1]. Phenotypic susceptibility testing shows, for the four R5-tropic HIV-2 isolates, a median EC50 for Cenicriviroc Mesylate of 0.39 nM (0.03, 0.33, 0.45 and 0.98 nM). The dual-tropic and the X4-tropic HIV-2 strains are resistant to Cenicriviroc Mesylate with EC50 at >1000 nM, and Maximum percentages of inhibition (MPI) at 33% and 4%, respectively[2].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Cenicriviroc Mesylate Related Antibodies
    In Vivo

    Cenicriviroc Mesylate (CVC) treatment leads to dose-related decrease in monocyte/macrophage recruitment, and achieving statistical significance at doses ≥20 mg/kg/day (p<0.05). Compare to the vehicle-control group, peritoneal lavage monocyte/macrophage counts are decreased by: 5.7%, 45.2%, 76.5% and 26.0% for Cenicriviroc Mesylate 5 twice daily (BID), Cenicriviroc Mesylate20 twice daily (BID), Cenicriviroc Mesylate100 BID, Cenicriviroc Mesylate 20 once-daily (QD), respectively. Exposure to Cenicriviroc Mesylate is dose-related and correlated with the decrease in monocyte/macrophage recruitment, with Cenicriviroc Mesylate appearing to be more effective when given BID versus QD, in line with the higher plasma concentrations achieved with BID dosing and the known short half-life in mice (~2 hours)[1].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
    Molecular Weight

    793.05

    Formula

    C42H56N4O7S2
    CAS No.
    Appearance

    Solid

    Color

    Light yellow to yellow

    SMILES

    O=C(/C1=C/C2=CC(C3=CC=C(OCCOCCCC)C=C3)=CC=C2N(CC(C)C)CCC1)NC4=CC=C([S@](CC5=CN=CN5CCC)=O)C=C4.OS(=O)(C)=O
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage

    4°C, sealed storage, away from moisture

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

    Solvent & Solubility
    In Vitro: 

    DMSO : 100 mg/mL (126.10 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.2610 mL 6.3048 mL 12.6095 mL
    5 mM 0.2522 mL 1.2610 mL 2.5219 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

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    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    10% Tween-80    80% (5% w/v Glucose Solution)

      Solubility: ≥ 10 mg/mL (12.61 mM); Clear solution

    • Protocol 2

      Add each solvent one by one:  5% DMSO    40% PEG300    5% Tween-80    50% Saline

      Solubility: 2.5 mg/mL (3.15 mM); Clear solution; Need ultrasonic

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

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    Dosing volume
    (per animal)

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    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
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    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 99.94%

    SDS (252 KB)

    COA (250 KB) HNMR (289 KB) LCMS (96 KB)

    Handling Instructions (2659 KB)
    References
    Cell Assay
    [1]

    Mouse monocyte migration in response to Cenicriviroc Mesylate (CVC) treatment is assessed ex vivo in triplicate. Thioglycollate (TG) is injected intraperitoneally into male C57BL/6 mice (n=3; 8 to 10 weeks of age) and activated macrophages are collected 48 hours later by peritoneal lavage. Cells are incubated for 2 hours in the presence of 1 μM Cenicriviroc Mesylate. Cells are harvested from the lower compartment and analyzed by flow cytometry to enumerate F4/80+CD11b+ macrophages. Results are analyzed using FlowJo software[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [1]

    Male C57BL/6 mice (n=44; 8 to 10 weeks of age) are allocated to receive treatments via oral gavage (PO) on Days 1 to 5 in the following groups: non-disease control, vehicle control twice daily (BID), Cenicriviroc Mesylate 5 mg/kg/day (CVC5) BID, Cenicriviroc Mesylate 20 mg/kg/day (CVC20) BID, Cenicriviroc Mesylate 100 mg/kg/day (CVC100) BID, Cenicriviroc Mesylate 20 mg/kg once-daily (QD). On Day 4, peritonitis is induced via IP injection of thioglycollate (TG) 3.85% (1 mL/animal) 2 hours post-dose in all groups except non-disease controls[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 1.2610 mL 6.3048 mL 12.6095 mL 31.5239 mL
    5 mM 0.2522 mL 1.2610 mL 2.5219 mL 6.3048 mL
    10 mM 0.1261 mL 0.6305 mL 1.2610 mL 3.1524 mL
    15 mM 0.0841 mL 0.4203 mL 0.8406 mL 2.1016 mL
    20 mM 0.0630 mL 0.3152 mL 0.6305 mL 1.5762 mL
    25 mM 0.0504 mL 0.2522 mL 0.5044 mL 1.2610 mL
    30 mM 0.0420 mL 0.2102 mL 0.4203 mL 1.0508 mL
    40 mM 0.0315 mL 0.1576 mL 0.3152 mL 0.7881 mL
    50 mM 0.0252 mL 0.1261 mL 0.2522 mL 0.6305 mL
    60 mM 0.0210 mL 0.1051 mL 0.2102 mL 0.5254 mL
    80 mM 0.0158 mL 0.0788 mL 0.1576 mL 0.3940 mL
    100 mM 0.0126 mL 0.0630 mL 0.1261 mL 0.3152 mL
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    Cenicriviroc Mesylate Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    Cenicriviroc497223-28-6TAK-652TBR-652TAK652TAK 652TBR652TBR 652CCRHIVCC chemokine receptorHuman immunodeficiency virusInhibitorinhibitorinhibit

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