KW 3902

Names

[ Name ]:
KW 3902

[Synonym ]:
KW 3902
MK-7418
1,3-Dnax

Biological Activity

[Description]:

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].

[Related Catalog]:

Research Areas >> Neurological Disease

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

[References]

[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.

Chemical & Physical Properties

[ Density]:
1.262g/cm3

[ Boiling Point ]:
578ºC at 760mmHg

[ Molecular Formula ]:
C₂₀H₂₈N₄O₂

[ Molecular Weight ]:
356.46200

[ Flash Point ]:
303.4ºC

[ Exact Mass ]:
356.22100

[ PSA ]:
72.68000

[ LogP ]:
2.78400

[ Vapour Pressure ]:
2.33E-13mmHg at 25°C

[ Index of Refraction ]:
1.605

MSDS

Click to get detail MSDS

Safety Information

[ Hazard Statements ]:
H413

[ RIDADR ]:
NONH for all modes of transport

Synthetic Route

Click to get detail synthetic route

Precursor & DownStream

Precursor

DownStream

Articles

The effects of multiple doses of rolofylline on the single-dose pharmacokinetics of midazolam in healthy subjects.

Am. J. Ther. 17(1) , 53-60, (2010)

Rolofylline is a potent, selective adenosine A1 receptor antagonist that was under development for the treatment of patients with acute decompensated heart failure and renal function impairment. This ...

The disconnect between phase II and phase III trials of drugs for heart failure.

Nat. Rev. Cardiol. 10(2) , 85-97, (2013)

Hospitalization for heart failure (HF) is a clinical entity associated with high postdischarge morbidity and mortality, yet few therapies are available to improve outcomes in patients with this condit...

Design and rationale of the PROTECT study: a placebo-controlled randomized study of the selective A1 adenosine receptor antagonist rolofylline for patients hospitalized with acute decompensated heart failure and volume overload to assess treatment effect on congestion and renal function.

J. Card. Fail. 16(1) , 25-35, (2010)

Current treatment for acute decompensated heart failure (ADHF) is associated with incomplete resolution of symptoms and signs, recurrent symptoms of heart failure in-hospital and after discharge and h...