Art. -Nr.: HY-14882

Cenicriviroc

(Synonyms: TAK-652; TBR-652)

7 Cited Publications

Kundenbewertung

Based on 7 publication(s) in Google Scholar

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

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Reinheit: 99.51%
CAS. Nr.: 497223-25-3
Formel: C₄₁H₅₂N₄O₄S
Molecular Weight:696.94

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Cenicriviroc Chemical Structure

CAS. Nr.: 497223-25-3

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (7)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Cenicriviroc (TAK-652) is an orally active, dual CCR2/CCR5 antagonist, also inhibits both HIV-1 and HIV-2, and displays potent anti-inflammatory and antiinfective activity^[1].

IC₅₀ & Target^[3]^[4]^[5]

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)

Alle CCR Isoform-spezifische Produkte anzeigen :

Alle HIV Isoform-spezifische Produkte anzeigen :

In Vitro

Cenicriviroc prevents human immunodeficiency virus type 1 (HIV-1) from cellular entry^[2]. Regarding the 4 R5 HIV-2 clinical isolates tested, effective concentration 50% EC₅₀ for cenicriviroc are 0.03, 0.33, 0.45 and 0.98 nM. The dual-tropic and the X4-tropic HIV-2 strains are resistant to cenicriviroc with EC₅₀ at >1000 nM, and MPI at 33% and 4%, respectively^[3].

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

In Vivo

Cenicriviroc (≥20 mg/kg/day) significantly reduces monocyte/macrophage recruitment in vivo. At these doses, cenicriviroc shows antifibrotic effects, with significant reductions in collagen deposition, and collagen type 1 protein and mRNA expression across the three animal models of fibrosis. In the NASH model, cenicriviroc significantly reduces the non-alcoholic fatty liver disease activity score. Cenicriviroc treatment has no notable effect on body or liver/kidney weight^[1].

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

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 497223-25-3
Appearance Solid
Molecular Weight 696.94
Formel C₄₁H₅₂N₄O₄S
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
Synonyms

TAK-652; TBR-652
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (7)

All In Vivo ImagingIFELISABio/Physico-chemical AssayWB

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Journal Impact Factor

Biomaterials

Nanoparticles retard immune cells recruitment in vivo by inhibiting chemokine expression. [Abstract]

2021 Jan;265:120392. PMID: 32992116

Cenicriviroc 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 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.
Cells

Human Liver Spheroids as a Model to Study Aetiology and Treatment of Hepatic Fibrosis. [Abstract]

2020 Apr 14;9(4):964. PMID: 32295224

Cenicriviroc 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.
Am J Physiol Cell Physiol

Cenicriviroc prevents dysregulation of astrocyte/endothelial cross talk induced by ischemia and HIV-1 via inhibiting the NLRP3 inflammasome and pyroptosis. [Abstract]

2024 Feb 1;326(2):C487-C504. PMID: 38145295

Cenicriviroc 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 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 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 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.
Antiviral Res

The chemokine receptor antagonist cenicriviroc inhibits the replication of SARS-CoV-2 in vitro. [Abstract]

2020 Oct;182:104902. PMID: 32739404
Sci Rep

Inhibition of intrahepatic monocyte recruitment by Cenicriviroc and extracellular matrix degradation by MMP1 synergistically attenuate liver inflammation and fibrogenesis in vivo. [Abstract]

2024 Jul 23;14(1):16897. PMID: 39043893
Eur J Immunol

Cenicriviroc, a CCR2/CCR5 antagonist, promotes the generation of type 1 regulatory T cells. [Abstract]

2024 Jul;54(7):e2350847. PMID: 38643381
bioRxiv

MAIT cell responses to S. aureus and sensitivity to HlgAB are modulated by activation and tissue-dependent virulence effects. [Abstract]

2026 Mar 19:2026.03.17.712383. PMID: 41890076

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 50 mg/mL (71.74 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Ethanol : 2 mg/mL (2.87 mM; ultrasonic and warming and heat to 60°C)

H₂O : < 0.1 mg/mL (insoluble)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.4348 mL

7.1742 mL

14.3484 mL

5 mM

0.2870 mL

1.4348 mL

2.8697 mL

10 mM

0.1435 mL

0.7174 mL

1.4348 mL

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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

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

Stock Solution Working Solution

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 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.08 mg/mL (2.98 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (2.98 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Protokoll

Animal Administration^[1]

Male C57BL/6 mice (n=44; 8-10 weeks of age) are allocated to receive treatments via oral gavage (PO) on Days 1-5 in the following groups: non-disease control, vehicle control twice daily (BID), Cenicriviroc 5 mg/kg/day (Cenicriviroc5) BID, Cenicriviroc 20 mg/kg/day (Cenicriviroc20) BID, Cenicriviroc 100 mg/kg/day (Cenicriviroc100) BID, Cenicriviroc20 QD, and positive control (corticosteroid known to reduce inflammation in a variety of animal models) 1 mg/kg QD. On Day 4, peritonitis is induced via IP injection of TG 3.85% (1 mL/animal) 2 hours post-dose in all groups except non-disease controls.

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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (277 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Lefebvre E, et al. Antifibrotic Effects of the Dual CCR2/CCR5 Antagonist Cenicriviroc in Animal Models of Liver and Kidney Fibrosis. PLoS One. 2016 Jun 27;11(6):e0158156 [Content Brief]

[2]. Kuwata T, et al. Incompatible Natures of the HIV-1 Envelope in Resistance to the CCR5 Antagonist Cenicriviroc and to Neutralizing Antibodies. Antimicrob Agents Chemother. 2015 Nov 2;60(1):437-5 [Content Brief]

[3]. Visseaux B, et al. Cenicriviroc, a Novel CCR5 (R5) and CCR2 Antagonist, Shows In Vitro Activity against R5 Tropic HIV-2 Clinical Isolates. PLoS One. 2015 Aug 6;10(8):e0134904 [Content Brief]

[4]. Lalezari J, et al. Safety, efficacy, and pharmacokinetics of TBR-652, a CCR5/CCR2 antagonist, in HIV-1-infected, treatment-experienced, CCR5 antagonist-naive subjects. J Acquir Immune Defic Syndr. 2011 Jun 1;57(2):118-25. [Content Brief]

[5]. Baba M, et al. TAK-652 inhibits CCR5-mediated human immunodeficiency virus type 1 infection in vitro and has favorable pharmacokinetics in humans. Antimicrob Agents Chemother. 2005 Nov;49(11):4584-91. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
Ethanol / DMSO	1 mM	1.4348 mL	7.1742 mL	14.3484 mL	35.8711 mL
DMSO	5 mM	0.2870 mL	1.4348 mL	2.8697 mL	7.1742 mL
	10 mM	0.1435 mL	0.7174 mL	1.4348 mL	3.5871 mL
	15 mM	0.0957 mL	0.4783 mL	0.9566 mL	2.3914 mL
	20 mM	0.0717 mL	0.3587 mL	0.7174 mL	1.7936 mL
	25 mM	0.0574 mL	0.2870 mL	0.5739 mL	1.4348 mL
	30 mM	0.0478 mL	0.2391 mL	0.4783 mL	1.1957 mL
	40 mM	0.0359 mL	0.1794 mL	0.3587 mL	0.8968 mL
	50 mM	0.0287 mL	0.1435 mL	0.2870 mL	0.7174 mL
	60 mM	0.0239 mL	0.1196 mL	0.2391 mL	0.5979 mL

Keywords

Cenicriviroc

7 Cited Publications

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Cenicriviroc

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Publications Citing Use of MedChemExpress (MCE) Cenicriviroc

Alle CCR Isoform-spezifische Produkte anzeigen

Alle HIV Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (7)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Cenicriviroc Related Classifications

HY-14882 Related Classifications