| Identification | Back 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 Properties | Back 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 Information | Back 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 | [Uses]
CAY10595 is a potent CRTH2/DP2 receptor antagonist that binds to the human receptor with a Ki of 10 nM. | [in vivo]
Administration of the DP2 antagonist CAY10595 slightly delays the development of CIA. Treatment with CAY10595 reduces IgG2a anti-CII levels without modification of IgG anti-CII levels[2]. | [IC 50]
DP: 10 nM (Ki) | [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). |
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| Company Name: |
BOC Sciences
|
| Tel: |
1-631-485-4226; 16314854226 |
| Website: |
https://www.bocsci.com |
| Company Name: |
cjbscvictory
|
| Tel: |
13348960310 |
| Website: |
https://www.weikeqi-biotech.com/ |
|