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Cenicriviroc CCR inhibitor

Name: Cenicriviroc
Brand: Selleck Chemicals
SKU: S8512
Availability: InStock
Rating: 5 (8 reviews)

Cat.No.S8512

Cenicriviroc is a potent, orally active dual inhibitor of CC chemokine receptor 2 (CCR2) and CCR5. This compound also inhibits HIV-1 and HIV-2 with potent anti-inflammatory and antiinfective activity.

Chemical Structure

Molecular Weight: 696.94

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Quality Control

Batch: Purity: 99.76%

99.76

Related Targets	PD-1/PD-L1 CXCR STING AhR Immunology & Inflammation related CD markers Interleukins Anti-infection Antioxidant COX
Other CCR Inhibitors	INCB3344 Vicriviroc Malate Adaptavir (DAPTA) ZK756326 2HCl BX471 (ZK-811752) RS102895 BMS-813160 SB-297006 R243 Vicriviroc maleate

Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Incubation Time	Activity Description	PMID
NIH/3T3	Function assay	1 hr	Displacement of [125I]-RANTES from CCR5 in mouse NIH/3T3 cells after 1 hr, IC50=0.00025μM.	29425816
VERO-E6	Function assay	48 hrs	Toxicity CC50 against VERO-E6 cells determined at 48 hours by high content imaging (same conditions as 2_LEY without exposure to 0.01 MOI SARS CoV-2 virus), CC50=11.73μM.	ChEMBL
Click to View More Cell Line Experimental Data

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (143.48 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 100 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

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: μL

Number of animals:

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.

Chemical Information, Storage & Stability

Molecular Weight	696.94	Formula	C₄₁H₅₂N₄O₄S	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	497223-25-3	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	TAK-652, 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

Mechanism of Action

Targets/IC₅₀/Ki	CCR2 CCR5 HIV-1 HIV-2
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 this compound at a concentration of 1 μM.
In vivo	Cenicriviroc significantly reduces monocyte/macrophage recruitment in vivo at doses >= 20 mg/kg/day (p < 0.05). At these doses, this compound 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, it significantly reduces the nonalcoholic fatty liver disease activity score (p < 0.05 vs. controls). This treatment has no notable effect on body or liver/kidney weight.
References	[1] https://pubmed.ncbi.nlm.nih.gov/21317794/ [2] https://pubmed.ncbi.nlm.nih.gov/27347680/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT06329310	Not yet recruiting	End Stage Renal Disease	Xeltis	July 2024	Not Applicable
NCT06190717	Recruiting	Diabetes\|End Stage Renal Disease	Sonavex Inc.	February 21 2024	Not Applicable
NCT06310174	Recruiting	Central Venous Catheter Exit Site Infection	Johns Hopkins University	December 22 2023	--
NCT06121115	Completed	Septic Shock\|Hypotension and Shock	Region Skane	October 3 2023	--
NCT05896735	Recruiting	Multiple Trauma/Injuries	Second Affiliated Hospital School of Medicine Zhejiang University	April 25 2023	--
NCT05751395	Not yet recruiting	Central Venous Catheter	Deutsche Interdisziplinäre Vereinigung für Intensiv- und Notfallmedizin	March 1 2023	--

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