A potent CRTH2/DP2 receptor antagonist that binds to the human receptor with a Ki value of 37 nM; R enantiomer of CAY10597 inhibits eosinophil chemotaxis induced by 13

CAY10597 – 10 mg

Brand:
Cayman
CAS:
916046-55-4
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} CAY10597, as a racemic mixture, is a potent CRTH2/DP2 receptor antagonist that binds to the human receptor with a Ki value of 37 nM.{15596} The R enantiomer is slightly more potent exhibiting Ki values of 23 and 22 nM at the human and murine CRTH2/DP2 receptor, respectively. The R enantiomer of CAY10597 inhibits eosinophil chemotaxis induced by 13,14-dihydro-15-keto-prostaglandin D2 with an IC50 value of 40 nM.{15596}  

 

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SKU: 10012539 - 10 mg Category:

Description

A potent CRTH2/DP2 receptor antagonist that binds to the human receptor with a Ki value of 37 nM; R enantiomer of CAY10597 inhibits eosinophil chemotaxis induced by 13,14-dihydro-15-keto-PGD2 with an IC50 value of 40 nM

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

Synonyms: 

Molecular weight: 416.8

CAS: 916046-55-4

Purity: ≥98%

Formulation: A crystalline solid

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

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