CAY10595

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. 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. 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.Formal Name: 5-chloro-1'-[5-chloro-2-fluorophenyl)methyl]-2,2',5'-trioxo-spiro[3H-indole-3,3'pyrrolidine]-1(2H)-acetic acid. CAS Number: 916047-16-0. Molecular Formula: C20H13Cl2FN2O5. Formula Weight: 451.2. Purity: >97%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMSO: 30 mg/ml, DMSO:PBS (pH 7.2) (1:10): 0.5 mg/ml, Ethanol: 25 mg/ml. SMILES: ClC1=CC=C(N(CC(O)=O)C(C23CC(N(CC4=C(F)C=CC(Cl)=C4)C3=O)=O)=O)C2=C1. InChi Code: InChI=1S/C20H13Cl2FN2O5/c21-11-1-3-14(23)10(5-11)8-25-16(26)7-20(19(25)30)13-6-12(22)2-4-15(13)24(18(20)29)9-17(27)28/h1-6H,7-9H2,(H,27,28). InChi Key: IXKFWNVFUXXEFY-UHFFFAOYSA-N.