Home>>Signaling Pathways>> Microbiology & Virology>> HIV>>Cenicriviroc

Cenicriviroc (Synonyms: TAK-652)

Catalog No.GC19101

Cenicriviroc (CVC) is an oral, dual CCR2/CCR5 antagonist with nanomolar potency against both receptors.

Products are for research use only. Not for human use. We do not sell to patients.

Cenicriviroc Chemical Structure

Cas No.: 497223-25-3

Size Price Stock Qty
1mg
$59.00
In stock
5mg
$164.00
In stock
10mg
$262.00
In stock
25mg
$525.00
In stock
50mg
$818.00
In stock

Tel:(909) 407-4943 Email: sales@glpbio.com

Customer Reviews

Based on customer reviews.

  • GlpBio Citations

    GlpBio Citations
  • Bioactive Compounds Premium Provider

    Bioactive Compounds Premium Provider

Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

View current batch:

Protocol

Cell experiment [1]:

Cell lines

human hepatocyte cell line(Huh7.5,Huh7.5JFH1)

Preparation Method

Huh7.5JFH1 cells were plated in 24-well format. After 24 hours, cells were incubated with cenicriviroc.The chemokines MIP-1 alpha MIP-1 beta, and RANTES/CCL5 were quantified in cell supernatants at day 1 and day 3 after addition of Cenicriviroc.

Reaction Conditions

Hepatocyte cell line were treated with Cenicriviroc (0.0025, 0.25, 25 ug/mL) for 24 h.

Applications

HCV core protein levels were significantly reduced in the presence of 0.25 and 25 ug/mL of cenicriviroc.MIP-1 beta expression at day 1 was somewhat lower in the presence of cenicriviroc compared to the no-drug control condition.

Animal experiment [2]:

Animal models

C57BL/6 mice

Preparation Method

Cenicriviroc was administered by oral gavage on Days 1–5. On Day 4, peritonitis was induced via IP injection of TG 3.85% (1 mL/animal) 2 hours post-dose.

Dosage form

5,20,100mg/kg/day, oral gavage

Applications

In vivo mouse model of peritonitis In the TG-induced model of peritonitis, Cenicriviroc treatment led to dose-related decreases in monocyte/macrophage recruitment, of similar or greater magnitude than those observed with dexamethasone.The most potent mediator of chemotaxis for activated macrophages, was reduced following pretreatment with Cenicriviroc at a concentration of 1μM.

References:

[1]. Blackard JT, Kong L, et al. CCR5 receptor antagonism inhibits hepatitis C virus (HCV) replication in vitro. PLoS One. 2019 Oct 29;14(10):e0224523. 

[2]. Lefebvre E, Moyle G, 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.

Background

Cenicriviroc (CVC) is an oral, dual CCR2/CCR5 antagonist with nanomolar potency against both receptors[1].

Cenicriviroc is a small-molecule chemokine receptor antagonist with highly potent and selective anti-human immunodeficiency virus type 1 (HIV-1) activity through antagonizing CCR5 as a coreceptor of HIV-1. Cenicriviroc also strongly antagonizes CCR2b, thereby it has potent anti-inflammatory and immunomodulatory effects[2].

Cenicriviroc is a selective inhibitor of SARS-CoV-2 replication.When VeroE6/TMPRSS2 cells were infected with SARS-CoV-2 and incubated in the absence of compounds for 3 days, the cells were completely destroyed by the virus-induced cytopathic effect (Fig. 1 B). Such cell destruction was not observed for the infected cells in the presence of 20 μM Cenicriviroc, although some morphological changes were identified[3].

Repeated intrathecal injections of Cenicriviroc in a dose-dependent manner alleviated neuropathic pain-related behaviors in rats after sciatic nerve injury. Cenicriviroc decreased the activation and/or infiltration of IBA-1-positive cells (microglia/macrophages) in the spinal cord and DRG, and satellite cells in the DRG, and likely as a consequence reduced the level of some important pronociceptive factors (IL-1beta, IL-6, IL-18, and CCL3). Importantly, from a clinical perspective, cenicriviroc enhanced the analgesic potency of morphine and buprenorphine. These beneficial behavioral effects may result, among others, from the influence of cenicriviroc on the mRNA level of opioid receptors (MOR, DOR, KOR, and NOR) at the DRG level. Our results provide the first evidence that simultaneous targeting of CCR2 and CCR5 using cenicriviroc may have great potential for use in neuropathic pain therapies, especially since it is already under clinical trials, though in other health concerns[3].

References:
[1]. Lefebvre E, Moyle G, 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.
[2].Okamoto M, Toyama M, et al. The chemokine receptor antagonist cenicriviroc inhibits the replication of SARS-CoV-2 in vitro. Antiviral Res. 2020 Oct;182:104902.
[3].Kwiatkowski K, Pawlik K, et al. Bidirectional Action of Cenicriviroc, a CCR2/CCR5 Antagonist, Results in Alleviation of Pain-Related Behaviors and Potentiation of Opioid Analgesia in Rats With Peripheral Neuropathy. Front Immunol. 2020 Dec 21;11:615327.

Chemical Properties

Cas No. 497223-25-3 SDF
Synonyms TAK-652
Canonical 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
Formula C41H52N4O4S M.Wt 696.94
Solubility DMSO : ≥ 107.5 mg/mL (135.55 mM) Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 1.4348 mL 7.1742 mL 14.3484 mL
5 mM 0.287 mL 1.4348 mL 2.8697 mL
10 mM 0.1435 mL 0.7174 mL 1.4348 mL
  • Molarity Calculator

  • Dilution Calculator

Mass
=
Concentration
x
Volume
x
MW*
 
 
 
**When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / CoA (available online).

Calculate

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

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.
3. All of the above co-solvents are available for purchase on the GlpBio website.

Reviews

Review for Cenicriviroc

Average Rating: 5 ★★★★★ (Based on Reviews and 24 reference(s) in Google Scholar.)

5 Star
100%
4 Star
0%
3 Star
0%
2 Star
0%
1 Star
0%
Review for Cenicriviroc

GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.

Required fields are marked with *

You may receive emails regarding this submission. Any emails will include the ability to opt-out of future communications.