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Rolofylline
SKU
HY-10965-10 mg
Category Reference compound
Tags Adenosine Receptor, GPCR/G Protein, Neurological Disease
$120 – $990
Products Details
Product 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].
Web ID
– HY-10965
Storage Temperature
– -20°C, 3 years (Powder)
Shipping
– Blue Ice
Applications
– Neuroscience-Neurodegeneration
Molecular Formula
– C20H28N4O2
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.
CAS Number
– 136199-02-5
Molecular Weight
– 356.46
Compound Purity
– 99.45
SMILES
– O=C(N1CCC)N(CCC)C2=C(N=C(C34CC(C5)CC3CC5C4)N2)C1=O
Clinical Information
– Phase 3
Research Area
– Neurological Disease
Solubility
– DMSO : 20 mg/mL (ultrasonic)
Target
– Adenosine Receptor
Pathway
– GPCR/G Protein
Product type
– Reference compound
Disclaimer: All products are for Research use only unless clearly stated otherwise on the product datasheet. Datasheets provided on the website are drafts for reference purpose only and you are requested to always refer to the hard copy included in the kit for your experimentation. Agdia Products are available for delivery only in Canada.