An orally bioavailable antagonist of CRTH2/DP2 (IC50 = 6 nM for the human receptor); selective for CRTH2/DP2 over DP1 in a radioligand binding assay (IC50 = 1

Setipiprant – 10 mg

Brand:
Cayman
CAS:
866460-33-5
Storage:
-20
UN-No:
Non-Hazardous - /

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).  

 

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SKU: 28291 - 10 mg Category:

Description

An orally bioavailable antagonist of CRTH2/DP2 (IC50 = 6 nM for the human receptor); selective for CRTH2/DP2 over DP1 in a radioligand binding assay (IC50 = 1,290 nM) and EP2 and EP4 in a β-arrestin assay (IC50s = 2,600 and >10,000 nM, respectively); inhibits PGD2-induced calcium flux in HEK293 cells expressing human CRTH2/DP2 (IC50 = 30 nM); inhibits PGD2-induced shape change in human eosinophils (IC50 = 235 nM)

Formal name: 8-fluoro-1,2,3,4-tetrahydro-2-(1-naphthalenylcarbonyl)-5H-pyrido[4,3-b]indole-5-acetic acid

Synonyms:  ACT-129968

Molecular weight: 402.4

CAS: 866460-33-5

Purity: ≥98%

Formulation: A solid

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