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CAY10595 Exclusive

Cayman Chemical Item Number 10012553

(CAS 916047-16-0)

CAY10595 (CAS 916047-16-0)

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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

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).

Formal Name 5-​chloro-​1'-​[5-​chloro-​2-​fluorophenyl)methyl]-​2,​2',​5'-​trioxo-​spiro[3H-​indole-​3,​3'pyrrolidine]-​1(2H)-​acetic acid
CAS Number 916047-16-0
Molecular Formula C20H13Cl2FN2O5
Formula Weight 451.2
Formulation A crystalline solid
Purity ≥97%
Stability 2 years
Storage -20°C
Shipping Room temperature in continental US; may vary elsewhere
SMILES
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ClC1=CC=C(N(CC(O)​=O)​C(C23CC(N(CC4=C(F)​C=CC(Cl)​=C4)​C3=O)​=O)​=O)​C2=C1

Background Reading

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).

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).
Size Price Quantity Subtotal
1 mg $50.00 $0.00
5 mg $225.00 $0.00
10 mg $400.00 $0.00
50 mg $1,750.00 $0.00
Bulk Contact
Cart Total $0.00

This product is available in custom sizes and/or larger quantities.

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Pricing updated 2012-05-25. Prices are subject to change without notice.

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Warning This product is not for human or veterinary use.

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