CAY10595 是一种有效的 CRTH2/DP2 受体拮抗剂，可与人类受体结合，Ki 为 10 nM。
| Cas No. | 916047-16-0 |
| 化学名 | 5-chloro-1'-[5-chloro-2-fluorophenyl)methyl]-2,2',5'-trioxo-spiro[3H-indole-3,3'pyrrolidine]-1(2H)-acetic acid |
| Canonical SMILES | ClC1=CC=C(N(CC(O)=O)C(C23CC(N(CC4=C(F)C=CC(Cl)=C4)C3=O)=O)=O)C2=C1 |
| 分子式 | C20H13Cl2FN2O5 |
| 分子量 | 451.2 |
| 溶解度 | DMF: 30 mg/ml,DMSO: 30 mg/ml,DMSO:PBS (pH 7.2) (1:10): 0.5 mg/ml,Ethanol: 25 mg/ml |
| 储存条件 | Store at -20°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 产品描述 | 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. |
m.cnreagent.com