Rolofylline
Product Specifications
UNSPSC 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].
Target Antigen
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 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.
Shipping Conditions
Blue Ice
Storage Conditions
-20°C, 3 years (Powder)
Product Datasheet
http://file.medchemexpress.com/batch_PDF/HY-10965/Rolofylline-DataSheet-MedChemExpress.pdf
Product MSDS
http://file.medchemexpress.com/batch_PDF/HY-10965/Rolofylline-SDS-MedChemExpress.pdf
Clinical Information
Phase 3
CAS Number
136199-02-5
Available Sizes
Curated Selection
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