Setipiprant(ACT129968) Datasheet DC Chemicals
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Cat.No DC8624
Name Setipiprant(ACT129968)

Chemical Properties

CAS 866460-33-5
Formula C24H19FN2O3
MW 402.42
Storage 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Biological activity

Description
Target: IC50 value: 6.0 nM Target: PGD2
In Vivo
In Vitro Setipiprant is an orally available, selective CRTH2 (chemoattractant receptor-homologous molecule expressed on T helper [Th]-2 cells) antagonist. CRTH2 is a G protein-coupled receptor for prostaglandin (PGD2). PGD2 is produced by the mast cells and is a key mediator in various inflammatory diseases, including allergy and asthma. Binding of PGD2 to CRTH2, which are expressed on the surface of blood-borne cells, induces chemotaxis of Th2 cells, basophils, and eosinophils, and stimulates cytokine release from these cells. Thus, antagonism of CRTH2 receptors is considered to be a promising therapeutic target for various allergic diseases and asthma.
Kinase Assay
Cell Assay
Animal Administration

References

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