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ChemicalBook--->CAS DataBase List--->916047-16-0

916047-16-0

916047-16-0 Structure

916047-16-0 Structure
IdentificationBack Directory
[Name]

CAY10595
[CAS]

916047-16-0
[Synonyms]

CAY10595
CAY10595,CAY-10595
CAY10595 Exclusive
IXKFWNVFUXXEFY-UHFFFAOYSA-N
Spiro[3H-indole-3,3'-pyrrolidine]-1(2H)-acetic acid, 5-chloro-1'-[(5-chloro-2-fluorophenyl)methyl]-2,2',5'-trioxo-
[Molecular Formula]

C20H13Cl2FN2O5
[MDL Number]

MFCD18427989
[MOL File]

916047-16-0.mol
[Molecular Weight]

451.23
Chemical PropertiesBack Directory
[storage temp. ]

Store at -20°C
[solubility ]

DMF: 30 mg/ml; DMSO: 30 mg/ml; DMSO:PBS (pH 7.2) (1:10): 0.5 mg/ml; Ethanol: 25 mg/ml
[form ]

A crystalline solid
Hazard InformationBack Directory
[Description]

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 PGD2.1 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.2 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.2
[References]

1. Hirai, H., Tanaka, K., Yoshie, O., et al. Prostaglandin D2 selectivity induces chemotaxis in T helper type 2 cells, eosinophils, and basophils via seven-transmembrane receptor CRTH2 J. Exp. Med. 193(2),255-261(2001).
2. Crosignani, S., Page, P., Missotten, M., et al. Discovery of a new class of potent, selective, and orally bioavailable CRTH2 (DP2) receptor antagonists for the treatment of allergic inflammatory diseases J. Med. Chem. 51,2227-2243(2008).
Spectrum DetailBack Directory
[Spectrum Detail]

CAY10595(916047-16-0)1HNMR
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