Home Immunology & Inflammation CXCR antagonist AMG 487

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AMG 487 CXCR antagonist

Cat.No.S8682

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 CXCR antagonist Chemical Structure

Chemical Structure

Molecular Weight: 603.59

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Quality Control

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

Chemical Information, Storage & Stability

Molecular Weight 603.59 Formula

C32H28F3N5O4

 Storage (From the date of receipt) 3 years -20°C powder
CAS No. 473719-41-4 -- Storage of Stock Solutions

Synonyms N/A 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

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (165.67 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 100 mg/mL

Water : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
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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.
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Mechanism of Action

Targets/IC50/Ki
CXCR3-CXCL10 [1]
(Cell-free assay)
8.0 nM
CXCR3-CXCL11 [1]
(Cell-free assay)
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]
References

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