Cenicriviroc

Catalog No.S8512 Batch:S851202

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Technical Data

Formula

C41H52N4O4S

Molecular Weight 696.94 CAS No. 497223-25-3
Solubility (25°C)* In vitro DMSO 100 mg/mL (143.48 mM)
Ethanol 100 mg/mL (143.48 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description Cenicriviroc is a potent, orally active dual inhibitor of CC chemokine receptor 2 (CCR2) and CCR5. Cenicriviroc also inhibits HIV-1 and HIV-2 with potent anti-inflammatory and antiinfective activity.
Targets
CCR2 [1] CCR5 [1] HIV-1 [1] HIV-2 [1]
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 Cenicriviroc at a concentration of 1 μM.[2]

In vivo

Cenicriviroc significantly reduces monocyte/macrophage recruitment in vivo at doses >= 20 mg/kg/day (p < 0.05). At these doses, Cenicriviroc 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, Cenicriviroc significantly reduces the nonalcoholic fatty liver disease activity score (p < 0.05 vs. controls). Cenicriviroc treatment has no notable effect on body or liver/kidney weight.[2]

Protocol (from reference)

Cell Assay:

[2]

  • Cell lines

    activated macrophages

  • Concentrations

    1 μM

  • Incubation Time

    2 h

  • Method

    TG is injected intraperitoneally into male C57BL/6 mice and activated macrophages are collected 48 hours later by peritoneal lavage. Chemotaxis is assayed using a Transwell1 Chamber with a 5 μm-pore size polycarbonate filter. Briefly, cells are incubated for 2 hours in the presence of 1 nM CCL2 and/or 1 μM Cenicriviroc (dissolved in dimethyl sulfoxide with 0.5% acetic acid and diluted 1:1000 with serum-free Roswell Park Memorial Institute-1640 medium and 0.5% bovine serum albumin). Cells are harvested from the lower compartment and analyzed by flow cytometry to enumerate F4/80+CD11b+ macrophages using a 3-laser BD FACSCanto. Results are analyzed using FlowJo software.

Animal Study:

[2]

  • Animal Models

    8–10 weeks old male C57BL/6 mice, 10–12 weeks old male Sprague-Dawley rats

  • Dosages

    5 mg/kg, 20 mg/kg, 100 mg/kg, 30 mg/kg

  • Administration

    Oral gavage, IP

Selleck's Cenicriviroc has been cited by 7 publications

C-C motif chemokine receptor 2 inhibition reduces liver fibrosis by restoring the immune cell landscape [ Int J Biol Sci, 2023, 19(8):2572-2587] PubMed: 37215993
Targeted Deletion of Rictor in BMSCs Reduces the Biological Activity of K7M2 Cells and Mitigates OS-Induced Bone Destruction [ Stem Cells, 2023, 41(6):672-683] PubMed: 37099695
Proteomic analysis reveals microvesicles containing NAMPT as mediators of radioresistance in glioma [ Life Science Alliance, 2023, 6(6)] PubMed: None
Proteomic analysis reveals microvesicles containing NAMPT as mediators of radioresistance in glioma [ Life Sci Alliance, 2023, 6(6)e202201680] PubMed: 37037593
Cancer-associated fibroblasts facilitate premetastatic niche formation through lncRNA SNHG5-mediated angiogenesis and vascular permeability in breast cancer [ Theranostics, 2022, 12(17):7351-7370] PubMed: 36438499
Deficiency of Lactoferrin aggravates lipopolysaccharide-induced acute inflammation via recruitment macrophage in mice [ Biometals, 2022, 1-14] PubMed: 35650365
C-reactive protein protects against acetaminophen-induced liver injury by preventing complement overactivation [ Cell Mol Gastroenterol Hepatol, 2021, S2352-345X(21)00191-0] PubMed: 34536564

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.