A potent CRTH2/DP2 receptor antagonist that binds to the human receptor with a Ki value of 10 nM; R enantiomer of CAY10595 inhibits eosinophil chemotaxis induced by 13

CAY10595 – 5 mg

Brand:
Cayman
CAS:
916047-16-0
Storage:
-20
UN-No:
Non-Hazardous - /

The biological effects of prostaglandin D2 (PGD2) are transduced by at least two 7-transmembrane G protein-coupled receptors, designated DP1 and CRTH2/DP2. In humans, CRTH2/DP2 is expressed on Th2 cells, eosinophils, and basophils where it mediates the chemotactic activity of PGD2.{9769} CAY10595, as a racemic mixture, is a potent CRTH2/DP2 receptor antagonist that binds to the human receptor with a Ki value of 10 nM.{15596} The R enantiomer of CAY10595 is significantly more potent exhibiting Ki values of 5.3 and 5 nM at the human and murine CRTH2/DP2 receptor, respectively. The R enantiomer of CAY10595 inhibits eosinophil chemotaxis induced by 13,14-dihydro-15-keto-PGD2 with an IC50 value of 7.3 nM.{15596}  

 

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SKU: 10012553 - 5 mg Category:

Description

A potent CRTH2/DP2 receptor antagonist that binds to the human receptor with a Ki value of 10 nM; R enantiomer of CAY10595 inhibits eosinophil chemotaxis induced by 13,14-dihydro-15-keto-PGD2 with an IC50 value of 7.3 nM

Formal name: 5-chloro-1′-[5-chloro-2-fluorophenyl)methyl]-2,2′,5′-trioxo-spiro[3H-indole-3,3’pyrrolidine]-1(2H)-acetic acid

Synonyms: 

Molecular weight: 451.2

CAS: 916047-16-0

Purity: ≥97%

Formulation: A crystalline solid

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

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