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

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

Cat. No.: HY-14882A Purity: 98.23% ee.: 98.31%
Handling Instructions

Cenicriviroc 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.

Cenicriviroc Mesylate Chemical Structure

Cenicriviroc Mesylate Chemical Structure

CAS No. : 497223-28-6

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 227 In-stock
Estimated Time of Arrival: December 31
1 mg USD 90 In-stock
Estimated Time of Arrival: December 31
5 mg USD 160 In-stock
Estimated Time of Arrival: December 31
10 mg USD 260 In-stock
Estimated Time of Arrival: December 31
25 mg USD 520 In-stock
Estimated Time of Arrival: December 31
50 mg USD 880 In-stock
Estimated Time of Arrival: December 31
100 mg   Get quote  
200 mg   Get quote  

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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

Cenicriviroc 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)

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].

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].

Clinical Trial
Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 107.5 mg/mL (135.55 mM)

*"≥" means soluble, but saturation unknown.

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
10 mM 0.1261 mL 0.6305 mL 1.2610 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (2.62 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (2.62 mM); Clear solution

*All of the co-solvents are provided by MCE.
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
Molecular Weight

793.05

Formula

C₄₂H₅₆N₄O₇S₂

CAS No.

497223-28-6

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere

Purity: 98.23% ee.: 98.31%

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Product Name:
Cenicriviroc Mesylate
Cat. No.:
HY-14882A
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Cenicriviroc Mesylate

Cat. No.: HY-14882A