Molecular structure of CAY10595, CAS Number: 916047-16-0
CAY10595 (CAS 916047-16-0)
Alternate Names:
5-chloro-1'-[5-chloro-2-fluorophenyl)methyl]-2,2',5'-trioxo-spiro[3H-indole-3,3'pyrrolidine]-1(2H)-acetic acid
Application:
CAY10595 is a DP2/CRTH2 receptor antagonist
CAS Number:
916047-16-0
Molecular Weight:
451.23
Molecular Formula:
C20H13Cl2FN2O5
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.
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SDS & Certificate of Analysis
The biological effects of prostaglandin D2 (PGD2) are transduced by at least two 7-transmembrane G protein-coupled receptors, designated CRTH2/DP2 and DP1. In humans, CRTH2/DP2 is expressed on Th2 cells, basophils and eosinophils where it mediates the chemotactic activity of PGD2 (1). CAY10595, as a racemic mixture, is a potent CRTH2/DP2 receptor antagonist that binds 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 and 5.3 nM at the murine and human 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).
CAY10595 (CAS 916047-16-0) References
- Prostaglandin D2 selectively induces chemotaxis in T helper type 2 cells, eosinophils, and basophils via seven-transmembrane receptor CRTH2. | Hirai, H., et al. 2001. J Exp Med. 193: 255-61. PMID: 11208866
- Discovery of a new class of potent, selective, and orally bioavailable CRTH2 (DP2) receptor antagonists for the treatment of allergic inflammatory diseases. | Crosignani, S., et al. 2008. J Med Chem. 51: 2227-43. PMID: 18318469
- Prostaglandin D2 regulates joint inflammation and destruction in murine collagen-induced arthritis. | Maicas, N., et al. 2012. Arthritis Rheum. 64: 130-40. PMID: 21898357
- Opposing roles of prostaglandin D2 receptors in ulcerative colitis. | Sturm, EM., et al. 2014. J Immunol. 193: 827-39. PMID: 24929001
- Expression of DP2 (CRTh2), a prostaglandin D₂ receptor, in human mast cells. | Moon, TC., et al. 2014. PLoS One. 9: e108595. PMID: 25268140
- The arachidonic acid metabolite 11β-ProstaglandinF2α controls intestinal epithelial healing: deficiency in patients with Crohn's disease. | Coquenlorge, S., et al. 2016. Sci Rep. 6: 25203. PMID: 27140063
- Prostaglandin D2 enhances lipid accumulation through suppression of lipolysis via DP2 (CRTH2) receptors in adipocytes. | Wakai, E., et al. 2017. Biochem Biophys Res Commun. 490: 393-399. PMID: 28623133
- CRTH2 promotes endoplasmic reticulum stress-induced cardiomyocyte apoptosis through m-calpain. | Zuo, S., et al. 2018. EMBO Mol Med. 10: PMID: 29335338
- Inhibition of CRTH2-mediated Th2 activation attenuates pulmonary hypertension in mice. | Chen, G., et al. 2018. J Exp Med. 215: 2175-2195. PMID: 29970474
- Crth2 receptor signaling down-regulates lipopolysaccharide-induced NF-κB activation in murine macrophages via changes in intracellular calcium. | Diwakar, BT., et al. 2019. FASEB J. 33: 12838-12852. PMID: 31518163
Inhibitor of:
DP2.Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
CAY10595, 1 mg | sc-223875 | 1 mg | $106.00 | |||
CAY10595, 5 mg | sc-223875A | 5 mg | $480.00 |