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LUF 5834

Names

[ CAS No. ]:
333962-91-7

[ Name ]:
LUF 5834

[Synonym ]:
2-Amino-4-(4-hydroxyphenyl)-6-[(2H-imidazol-2-ylmethyl)sulfanyl]-3,5-pyridinedicarbonitrile
3,5-Pyridinedicarbonitrile, 2-amino-4-(4-hydroxyphenyl)-6-[(2H-imidazol-2-ylmethyl)thio]-
LUF5834
2-amino-4-(4-hydroxyphenyl)-6-(1H-imidazol-2-ylmethylsulfanyl)pyridine-3,5-dicarbonitrile

Biological Activity

[Description]:

LUF5834 is a selective A2B adenosine receptor (A2BR) partial agonist (EC50 = 12 nM). LUF5834 is also a partial A1/A2A adenosine receptor agonist (lacking selectivity) with Ki values of 2.6 and 28 nM, respectively[1][2].

[Related Catalog]:

Research Areas >> Others
Signaling Pathways >> GPCR/G Protein >> Adenosine Receptor

[Target]

A2BR:12 nM (EC50)

A2AR:28 nM (Ki)

A1R:2.6 nM (Ki)


[References]

[1]. Beukers MW, et al. New, non-adenosine, high-potency agonists for the human adenosine A2B receptor with an improved selectivity profile compared to the reference agonist N-ethylcarboxamidoadenosine. J Med Chem. 2004 Jul 15;47(15):3707-9.  

[2]. Lane JR, et al. A novel nonribose agonist, LUF5834, engages residues that are distinct from those of adenosine-like ligands to activate the adenosine A(2a) receptor. Mol Pharmacol. 2012 Mar;81(3):475-87.  

Chemical & Physical Properties

[ Density]:
1.5±0.1 g/cm3

[ Boiling Point ]:
655.8±65.0 °C at 760 mmHg

[ Molecular Formula ]:
C17H12N6OS

[ Molecular Weight ]:
348.38

[ Flash Point ]:
350.4±34.3 °C

[ Exact Mass ]:
348.079315

[ LogP ]:
2.75

[ Vapour Pressure ]:
0.0±2.0 mmHg at 25°C

[ Index of Refraction ]:
1.753

Related Compounds