Products for Research Use Only

Setipiprant

CAT: 0013-GTR19159322-01Size: 500 mgDry Ice: NoHazardous: No
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CAT#:0013-GTR19159322-01Size:500 mg
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Description
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.
CAS Number
866460-33-5
Product Name Alternative
ACT-129968 | ACT 129968 | KYTH 105 | Setipiprant
Purity
>98% (HPLC)
Solubility
DMSO : ≥ 36 mg/mL; 89.46 mM
Smiles
C1CN (CC2=C1N (C3=C2C=C (C=C3) F) CC (=O) O) C (=O) C4=CC=CC5=CC=CC=C54
Molecular Formula
C24H19FN2O3
Molecular Weight
402.42
Storage Conditions
Storage temperature: -20°C. Stability: ≥ 2 years
Notes
For research use only.
Other Product Names
2- (2- (1-naphthoyl) -8-fluoro-1,2,3,4-tetrahydro-5H-pyrido[4,3-b]indol-5-yl) acetic acid