Rolofylline

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]

Product Name Alternative

KW-3902

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Adenosine Receptor

Type

Reference compound

Related Pathways

GPCR/G Protein

Applications

Neuroscience-Neurodegeneration

Field of Research

Neurological Disease

Assay Protocol

https://www.medchemexpress.com/rolofylline.html

Purity

99.68

Solubility

DMSO : 20 mg/mL (ultrasonic)

Smiles

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

Molecular Formula

C20H28N4O2

Molecular Weight

356.46

Precautions

H302, H315, H319, H335

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.