PSB 0788

Names

[ Name ]:
PSB 0788

[Synonym ]:
5-Nonyloxytryptamine oxalate

Biological Activity

[Description]:

PSB-0788 (compound 17), xanthine-8-yl-benzenesulfonamide derivative, is a new selective high-affinity A2B antagonist with IC50 value of 3.64 nM and Ki value of 0.393 nM, respeactively. PSB-0788 (compound 17) can be used for the research for chronic inflammatory lung diseases[1].

[Related Catalog]:

Research Areas >> Cancer

Research Areas >> Infection

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

[Target]

IC50: 3.64 nM (A2BAdoR); Ki: 0.393 nM (human, A2B); >1000 nM ( A3 human recombinant); 333 nM ( A2A human recombinant); 1730 nM ( A2A rat brain striatal membranes); 2240 nM ( A1 human recombinant); 386 nM ( A1 rat brain cortical membranes))[1].[1]

[In Vitro]

PSB-0788 (compound 17) has high potency at the A2BAdoR with IC50 value of 3.64 nM. PSB-0788 (compound 17) has good profile of affinity and selectivity (Ki: 0.393 nM ( A2B human recombinant); >1000 nM ( A3 human recombinant); 333 nM ( A2A human recombinant); 1730 nM ( A2A rat brain striatal membranes); 2240 nM ( A1 human recombinant); 386 nM ( A1 rat brain cortical membranes))[1].

[References]

[1]. Thomas Borrmann, et al. 1-alkyl-8-(piperazine-1-sulfonyl)phenylxanthines: development and characterization of adenosine A2B receptor antagonists and a new radioligand with subnanomolar affinity and subtype specificity. J Med Chem. 2009 Jul 9;52(13):3994-4006.

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₅H₂₇ClN₆O₄S

[ Molecular Weight ]:
543.03800

[ Exact Mass ]:
542.15000

[ PSA ]:
132.54000

[ LogP ]:
3.60640

Related Compounds

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