• Product NameSetipiprant
• Brief DescriptionInhibitors
• Purification98.00%
• Biological ActivitySetipiprant is an orally available, selective CRTH2 antagonist. CRTH2 is a G protein-coupled receptor for PGD2. IC50 value: 6.0 nM Target: PGD2 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.
• Target NameGPR antagonist
• CAS No. 866460-33-5
• Calculated MW 402.42
• Formulation C24H19FN2O3
• Storage 3 years -20˚C powder;2 years -80˚C in solvent;

• Research Area:Others
  SMILES:C1CN(CC2=C1N(C3=C2C=C(C=C3)F)CC(=O)O)C(=O)C4=CC=CC5=CC=CC=C54
  Pathways:Endocrinology/Hormones
  Receptor:CRTh2
  Boling pt:
  Melting pt:
  Solubility:DMSO: 36 mg/mL
  Appearance:
  Remark:For obtaining a higher solubility , please warm the tube at 37 ˚C and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20 ˚C for several month.

1. Diamant Z., et al. Setipiprant, a selective CRTH2 antagonist, reduces allergen-induced airway responses in allergic asthmatics. Clin Exp Allergy. 2014 Aug;44(8):1044-52.

• Flow Cytometry (FCM) General Protocol
• Immunofluorescence(IC)
• Immunohistochemistry(Polymer)
• Western Blotting