A CRTH2/DP2 antagonist (IC50s = 9.58

LAS191859 – 500 µg

Brand:
Cayman
CAS:
1420071-13-1
Storage:
-20
UN-No:
Non-Hazardous - /

LAS191859 is a potent antagonist of CRTH2/DP2 with IC50 values of 9.58, 14, 15.5, and 7.6 nM for recombinant human, rat, mouse, and guinea pig CRTH2/DP2 receptors, respectively.{31718} It is selective for CRTH2/DP2 over a panel of 65 enzymes, ion channels, and transporters with 50s = 2 and 8.2 nM in isolated eosinophils and whole blood, respectively) and eosinophil chemotaxis (IC50 = 1.3 nM) induced by prostaglandin D2 (PGD2; Item No. 12010) binding to CRTH2/DP2. Oral administration of LAS191859 reduces PGD2-induced systemic eosinophilia in guinea pigs (ID50 = 131 μg/kg).  

 

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Description

A CRTH2/DP2 antagonist (IC50s = 9.58, 14, 15.5, and 7.6 nM for recombinant human, rat, mouse, and guinea pig CRTH2/DP2 receptors, respectively); selective for CRTH2/DP2 over a panel of 65 enzymes, ion channels, and transporters with 2-induced shape change of eosinophils (IC50s = 2 and 8.2 nM in isolated eosinophils and whole blood, respectively) and eosinophil chemotaxis (IC50 = 1.3 nM); reduces PGD2-induced systemic eosinophilia in guinea pigs (ID50 = 131 μg/kg)

Formal name: 1-[2-[[(cyclopropylcarbonyl)ethylamino]methyl]-4-(trifluoromethyl)phenyl]-6-methyl-1H-pyrrolo[2,3-b]pyridine-3-acetic acid

Synonyms: 

Molecular weight: 459.5

CAS: 1420071-13-1

Purity: ≥98%

Formulation: A crystalline solid

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

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