A CRTH2/DP2 receptor antagonist (Kd = 1.14 nM) with a relatively slow dissociation rate (half-life = 14.4 minutes); inhibits PGD2-stimulated human eosinophil shape change in whole blood assays and PGD2-induced cytokine release in human Th2 cells

Fevipiprant – 500 µg

Brand:
Cayman
CAS:
872365-14-5
Storage:
-20
UN-No:
Non-Hazardous - /

Fevipiprant is a prostaglandin D2 (PGD2; Item No. 12010) receptor antagonist with a Kd value of 1.14 nM for CRTH2/DP2 and a relatively slow dissociation from this receptor (half-life = 14.4 minutes).{32112} It has been shown to inhibit PGD2-stimulated human eosinophil shape change in whole blood assays (IC50 = 0.44 nM) and to inhibit PGD2-induced cytokine release in human Th2 cells (IC50s = 2.56 and 1.4 nM for IL-5 and IL-13, respectively).{32112} This compound has undergone testing in a phase II clinical study in uncontrolled allergic asthma.{32111}  

 

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Description

A CRTH2/DP2 receptor antagonist (Kd = 1.14 nM) with a relatively slow dissociation rate (half-life = 14.4 minutes); inhibits PGD2-stimulated human eosinophil shape change in whole blood assays and PGD2-induced cytokine release in human Th2 cells

Formal name: 2-methyl-1-[[4-(methylsulfonyl)-2-(trifluoromethyl)phenyl]methyl]-1 H -pyrrolo[2,3b]pyridine-3-acetic acid

Synonyms:  NVP-QAW039|QAW039

Molecular weight: 426.4

CAS: 872365-14-5

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Immunology & Inflammation|Adaptive Immunity||Research Area|Immunology & Inflammation|Inflammatory Lipid Mediators|Prostaglandins||Research Area|Immunology & Inflammation|Innate Immunity||Research Area|Lipid Biochemistry|Cyclooxygenase Pathway

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