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prostaglandin D2(PGD2) inhibitor

Names

[ CAS No. ]:
885066-67-1

[ Name ]:
prostaglandin D2(PGD2) inhibitor

[Synonym ]:
Benzeneacetic acid, 3-[6-[[2-(2,4-dichlorophenyl)ethyl]amino]-2-methoxy-4-pyrimidinyl]-α,α-dimethyl-
2-[3-(6-{[2-(2,4-Dichlorophenyl)ethyl]amino}-2-methoxy-4-pyrimidinyl)phenyl]-2-methylpropanoic acid

Biological Activity

[Description]:

PGD2-IN-1 is an antagonist of DP extracted from patent WO 2006044732 A2, example 15 (d); has an IC50 of 0.3 nM.

[Related Catalog]:

Signaling Pathways >> Others >> Others
Research Areas >> Inflammation/Immunology

[Target]

IC50: 0.3 nM[1]


[In Vitro]

Prostaglandin D2 (PGD2) is a major inflammatory mediator implicated in asthma and allergic rhinitis. It is largely produced as the major cyclooxygenase metabolite upon allergen-provoked degranulation from mast cells. Blockage of PGD2 using DP antagonistshave been shown to be effective at alleviating the symptoms of allergic rhinitis in multiple species and more specifically have been shown to inhibit the antigen-induced nasal congestion[1].

[References]

[1]. Patent: WO/2006/044732A2

[2]. Mu L, et al. Understanding DP receptor antagonism using a CoMSIA approach. Bioorg Med Chem Lett. 2011 Jan 1;21(1):66-75.


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Chemical & Physical Properties

[ Density]:
1.3±0.1 g/cm3

[ Boiling Point ]:
682.1±65.0 °C at 760 mmHg

[ Molecular Formula ]:
C23H23Cl2N3O3

[ Molecular Weight ]:
460.353

[ Flash Point ]:
366.3±34.3 °C

[ Exact Mass ]:
459.111633

[ LogP ]:
6.28

[ Appearance of Characters ]:
white solid

[ Vapour Pressure ]:
0.0±2.2 mmHg at 25°C

[ Index of Refraction ]:
1.622

[ Storage condition ]:
-20℃

Related Compounds