AMG 487

Catalog No.S8682 Batch:S868201

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Technical Data

Formula

C32H28F3N5O4
Molecular Weight 603.59 CAS No. 473719-41-4
Solubility (25°C)* In vitro DMSO 100 mg/mL (165.67 mM)
Ethanol 100 mg/mL (165.67 mM)
Water Insoluble
In vivo (Add solvents to the product individually and in order)
5% DMSO 95% Corn oil
2.5mg/ml
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
5.0mg/ml
* <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.)

Preparing Stock Solutions

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 (from reference)

Cell Assay:

[2]
  • 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.
Animal Study:

[3]
  • Animal Models

    DBA/1J mice

  • Dosages

    5 mg/kg

  • Administration

    IP

Selleck's AMG 487 has been cited by 1 publication

Delamanid suppresses CXCL10 expression via regulation of JAK/STAT1 signaling and correlates with reduced inflammation in tuberculosis patients [ Front Immunol, 2022, 13:923492] PubMed: 36426362

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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.