AMG 487

For research use only.

Catalog No.S8682

AMG 487 Chemical Structure

CAS No. 473719-41-4

AMG 487 is an orally active and selective CXC chemokine receptor 3 (CXCR3) antagonist that inhibits the binding of IP-10 (CXCL10) and ITAC (CXCL11) to CXCR3 with IC50 of 8.0 nM and 8.2 nM, respectively.

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Biological Activity

Description AMG 487 is an orally active and selective CXC chemokine receptor 3 (CXCR3) antagonist that inhibits the binding of IP-10 (CXCL10) and ITAC (CXCL11) to CXCR3 with IC50 of 8.0 nM and 8.2 nM, respectively.
Targets
CXCR3-CXCL10 [1]
(Cell-free assay)
CXCR3-CXCL11 [1]
(Cell-free assay)
8.0 nM 8.2 nM
In vitro

AMG487 is the targeted blocker of chemokine receptor CXCR3 and improves inflammatory symptoms by blocking the inflammatory cycle. AMG487 significantly affects DC maturity in vitro and function leading to impaired T cell activation, inducing DCs to have characteristics similar to tolerogenic DCs. AMG487 may directly play an immunomodulatory role during DC development and functional shaping.[2]

In vivo

AMG487 exhibits the antiarthritic effects in DBA/1J mice bearing collageninduced arthritis (CIA).[3]

Protocol

Cell Research:

[2]

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  • Cell lines: Murine bone marrow-derived DCs (BMDCs)
  • Concentrations: 3 μM, 15 μM, 30 μM, 60 μM
  • Incubation Time: over 6 days
  • Method:

    For the analysis of the toxic effect of AMG487 on bone marrow cells and the effect of AMG487 on BMDC development, the bone marrow cells are exposed to AMG487 (3 μM, 15 μM, 30 μM, and 60 μM) from day 0, and AMG487 is supplemented with appropriate amounts every 3 days. The cells are washed twice before adding LPS to induce maturation. To investigate the effect of AMG487 on BMDC activation, we add various concentrations of AMG487 (10 μM, 30 μM, and 60 μM) only on day 6 along with the LPS. Equal amounts of the vehicle are added as a control in each case.


    (Only for Reference)
Animal Research:

[3]

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  • Animal Models: DBA/1J mice
  • Dosages: 5 mg/kg
  • Administration: IP
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (165.67 mM)
Water Insoluble
Ethanol ''100 mg/mL

* 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.

Chemical Information

Molecular Weight 603.59
Formula

C32H28F3N5O4

CAS No. 473719-41-4
Storage powder
in solvent
Synonyms N/A

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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CXCR Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID