Setipiprant

Research use only, not for human use.

Setipiprant is an orally available, selective CRTH2 antagonist (IC50: 6.0 nM). CRTH2 is a G protein-coupled receptor for prostaglandin (PGD2).

Setipiprant is an orally available, selective CRTH2 antagonist (IC50: 6.0 nM). 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.(In Vitro):Setipiprant (0-10 μM; 90 min) interacts with hCRTH2 receptor in the absence and presence of Human Serum Albumin (HSA) in the assay buffer with IC50 values of 6 and 340 nM, respectively.Setipiprant (0-10 μM; 5-20 min) inhibits hCRTH2 receptor based intracellular calcium liberation, intracellular cAMP and shape change of human eosinophils with IC50 values of 30, 80 and 235 nM, respectively.Setipiprant (0-10 μM) inhibits prostanoid receptors hDP1, hEP2 and hEP4 with IC50 values of 1290, 2600 and ＞10000 nM, respectively.(In Vivo):Pharmacokinetic Properties of Setipiprant in Rats and Dogs.

Setipiprant (0-10 μM; 90 min) interacts with hCRTH2 receptor in the absence and presence ofHuman Serum Albumin (HSA) in the assay buffer with IC50 values of 6 and 340 nM, respectively.Setipiprant (0-10 μM; 5-20 min) inhibits hCRTH2 receptor based intracellular calcium liberation, intracellular cAMP and shape change of human eosinophils with IC50 values of 30, 80 and 235 nM, respectively.Setipiprant (0-10 μM) inhibits prostanoid receptors hDP1, hEP2 and hEP4 with IC50 values of 1290, 2600 and ＞10000 nM, respectively.

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ACT-129968 | ACT 129968 | KYTH 105 | Setipiprant

Others

Other Targets

CRTh2

Inflammation/Immunology

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866460-33-5

402.42

C24H19FN2O3

>98% (HPLC)

DMSO : ≥ 36 mg/mL; 89.46 mM

C1CN(CC2=C1N(C3=C2C=C(C=C3)F)CC(=O)O)C(=O)C4=CC=CC5=CC=CC=C54

2-(2-(1-naphthoyl)-8-fluoro-1,2,3,4-tetrahydro-5H-pyrido[4,3-b]indol-5-yl)acetic acid

(-20℃)

With Ice Pack

≥ 2 years