Rolofylline (Standard)

Rolofylline (Standard) is the analytical standard of Rolofylline. This product is intended for research and analytical applications. Rolofylline (KW-3902) is a potent, selective adenosine A1 receptor antagonist that is under development for the treatment of patients with acute congestive heart failure and renal impairment. Rolofylline is metabolized primarily to the pharmacologically active M1-trans and M1-cis metabolites by cytochrome P450 (CYP450) [1]. Rolofylline is alleviating the presynaptic dysfunction and restores neuronal activity as well as dendritic spine levels in vitro, is an interesting candidate to combat the hypometabolism and neuronal dysfunction associated with Tau-induced neurodegenerative diseases[2].

Product Specifications

CAS Number

[136199-02-5]

UNSPSC

12352100

Target

Adenosine Receptor; Reference Standards

Related Pathways

GPCR/G Protein; Others

Field of Research

Neurological Disease

Smiles

O=C(N1CCC)N(CCC)C2=C(N=C(C34CC(C5)CC3CC5C4)N2)C1=O

Molecular Formula

C20H28N4O2

Molecular Weight

356.46

References & Citations

[1]Stroh M, et al. Simultaneous pharmacokinetic model for rolofylline and both M1-trans and M1-cis metabolites. AAPS J. 2013 Apr;15 (2) :498-504.|[2]Dennissen FJ, et al. Adenosine A1 receptor antagonist rolofylline alleviates axonopathy caused by human Tau ΔK280. Proc Natl Acad Sci U S A. 2016 Oct 11;113 (41) :11597-11602. Epub 2016 Sep 26.