Formulation: A solid
Formal Name: 8-fluoro-1,2,3,4-tetrahydro-2-(1-naphthalenylcarbonyl)-5H-pyrido[4,3-b]indole-5-acetic acid
Purity: ≥98%
Formula Markup: C24H19FN2O3
Formula Weight: 402,4
Shelf life (days): 1460
CAS Number: 866460-33-5
Notes: Setipiprant is an orally bioavailable antagonist of the prostaglandin D2 (PGD2; Item No. 12010) receptor CRTH2/DP2 (IC50 = 6 nM for the human receptor).{42901} It is selective for CRTH2/DP2 over DP1 in a radioligand binding assay (IC50 = 1,290 nM) and the prostaglandin E2 (PGE2; Item No. 14010) receptor subtypes EP2 and EP4 in a β-arrestin assay (IC50s = 2,600 and >10,000 nM, respectively). Setipiprant inhibits PGD2-induced calcium flux in HEK293 cells expressing human CRTH2/DP2 (IC50 = 30 nM) and PGD2-induced shape change in human eosinophils (IC50 = 235 nM).