CAY10595

Product Name: CAY10595
CAS No.: 916047-16-0
Chemical Name: CAY10595
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-
CBNumber: CB52590436
Molecular Formula: C20H13Cl2FN2O5
Formula Weight: 451.23
MOL File: 916047-16-0.mol

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CAY10595 Property

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

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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

Cayman Chemical

Product number: 10012553
Product name: CAY10595
Purity: ≥97%
Packaging: 1mg
Price: $66
Updated: 2024/03/01

Cayman Chemical

Product number: 10012553
Product name: CAY10595
Purity: ≥97%
Packaging: 5mg
Price: $291
Updated: 2024/03/01

Cayman Chemical

Product number: 10012553
Product name: CAY10595
Purity: ≥97%
Packaging: 10mg
Price: $516
Updated: 2024/03/01

AK Scientific

Product number: 1879CW
Product name: 2-[5-Chloro-1'-[(5-chloro-2-fluorophenyl)methyl]-2,2',5'-trioxospiro[indole-3,3'-pyrrolidine]-1-yl]aceticacid
Packaging: 10mg
Price: $672
Updated: 2021/12/16

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CAY10595 Chemical Properties,Usage,Production

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 K_i value of 10 nM.² The R enantiomer of CAY10595 is significantly more potent exhibiting K_i 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).

CAY10595 Preparation Products And Raw materials

Raw materials

Preparation Products

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CAY10595 Suppliers

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916047-16-0, CAY10595Related Search:

CAY10595

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-

CAY10595,CAY-10595

916047-16-0