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.
Citations
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Chemical Properties
CAS No.
916047-16-0
Chemical Name
5-chloro-1'-[5-chloro-2-fluorophenyl)methyl]-2,2',5'-trioxo-spiro[3H-indole-3,3'pyrrolidine]-1(2H)-acetic acid
SMILES
ClC1=CC=C(N(CC(O)=O)C(C23CC(N(CC4=C(F)C=CC(Cl)=C4)C3=O)=O)=O)C2=C1
Molecular Formula
C20H13Cl2FN2O5
Molecular Weight
451.2
Solubility
DMF: 30 mg/ml,DMSO: 30 mg/ml,DMSO:PBS (pH 7.2) (1:10): 0.5 mg/ml,Ethanol: 25 mg/ml
Storage
Store at -20°C
General tips
Select a suitable solvent according to the product solubility data. Once prepared, aliquot the stock solution to avoid repeated freeze-thaw cycles.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Shipping Condition
Evaluation samples are shipped with blue ice. Other available sizes are shipped at room temperature or with blue ice upon request.
CalculatorsMolarity / Dilution / Molecular Weight / Unit Conversion / In Vivo Formulation / Solubility
g/mol
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