Setipiprant

Setipiprant

CAT N°: 28291
Price:

From 74.00 62.90

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 ?-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).

Territorial Availability: Available through Bertin Technologies only in France

  • Synonyms
    • 8-fluoro-1,2,3,4-tetrahydro-2-(1-naphthalenylcarbonyl)-5H-pyrido[4,3-b]indole-5-acetic acid
  • Correlated keywords
    • 1263765-62-3 ACT129968 KYTH-105 KYTH105 CRTH-2 DP-1 2 PGD-2 PGE-2 EP-2 4 HEK-293
  • Product Overview:
    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 ?-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).

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