Home Immunology & Inflammation CXCR antagonist AMG 487 For research use only.

AMG 487

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.

AMG 487 Chemical Structure

AMG 487 Chemical Structure

CAS: 473719-41-4

Selleck's AMG 487 has been cited by 1 publication

Purity & Quality Control

Batch: S868201 DMSO] 100 mg/mL] false] Ethanol] 100 mg/mL] false] Water] Insoluble] false Purity: 99.86%
99.86

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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
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]
Cell Research 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.
In Vivo
In vivo

AMG487 exhibits the antiarthritic effects in DBA/1J mice bearing collageninduced arthritis (CIA).[3]
Animal Research Animal Models DBA/1J mice
Dosages 5 mg/kg
Administration IP

Chemical lnformation & Solubility

Molecular Weight 603.59 Formula

C32H28F3N5O4
CAS No. 473719-41-4 SDF --
Smiles CCOC1=CC=C(C=C1)N2C(=O)C3=CC=CN=C3N=C2C(C)N(CC4=CC=CN=C4)C(=O)CC5=CC=C(OC(F)(F)F)C=C5
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 100 mg/mL ( (165.67 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 100 mg/mL

Water : Insoluble


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In vivo
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