CAY10595

Names

[ Name ]:
CAY10595

[Synonym ]:
[5-Chloro-1'-(5-chloro-2-fluorobenzyl)-2,2',5'-trioxospiro[indole-3,3'-pyrrolidin]-1(2H)-yl]acetic acid
Spiro-indolinone analogue,71
Spiro[3H-indole-3,3'-pyrrolidine]-1(2H)-acetic acid, 5-chloro-1'-[(5-chloro-2-fluorophenyl)methyl]-2,2',5'-trioxo-

Biological Activity

[Description]:

CAY10595 is a potent CRTH2/DP2 receptor antagonist that binds to the human receptor with a Ki of 10 nM.

[Related Catalog]:

Signaling Pathways >> GPCR/G Protein >> Prostaglandin Receptor

Research Areas >> Inflammation/Immunology

[Target]

CRTH2/DP2 Receptor:10 nM (Ki)

[In Vitro]

CAY10595 (compound 71) is a potent CRTH2/DP2 receptor antagonist that binds to the human receptor with a Ki of 10 nM[1].

[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].

[References]

[1]. Crosignani S, 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. 2008 Apr 10;51(7):2227-43.

[2]. Maicas N, et al. Prostaglandin D2 regulates joint inflammation and destruction in murine collagen-induced arthritis. Arthritis Rheum. 2012 Jan;64(1):130-40.

[Related Small Molecules]

Dinoprostone | Prostaglandin E1 | E7046 | ONO-AE3-208 | PF 04418948 | Fevipiprant | grapiprant | TG6-10-1 | Taprenepag | GW 627368 | MRE-269 | Ramatroban | AH 6809 | Laropiprant | AZD1981

Chemical & Physical Properties

[ Density]:
1.7±0.1 g/cm3

[ Boiling Point ]:
810.1±65.0 °C at 760 mmHg

[ Molecular Formula ]:
C₂₀H₁₃Cl₂FN₂O₅

[ Molecular Weight ]:
451.232

[ Flash Point ]:
443.8±34.3 °C

[ Exact Mass ]:
450.018555

[ PSA ]:
94.99000

[ LogP ]:
3.37

[ Vapour Pressure ]:
0.0±3.0 mmHg at 25°C

[ Index of Refraction ]:
1.705

Related Compounds

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