Tonapofylline
Tonapofylline (BG 9928) is an orally active and selective adenosine A1 receptor antagonist with a Ki of 7.4 nM for human adenosine A1 receptor (hA1), which displays 915-fold selectivity versus human adenosine A2A receptor and 12-fold selectivity versus human adenosine A2B receptor and is used in development for the treatment of heart failure[1][2].
Product Specifications
CAS Number
340021-17-2
Product Name Alternative
BG 9928
UNSPSC
12352005
Target
Adenosine Receptor
Type
Reference compound
Related Pathways
GPCR/G Protein
Applications
Neuroscience-Neuromodulation
Field of Research
Metabolic Disease; Cardiovascular Disease
Assay Protocol
https://www.medchemexpress.com/tonapofylline.html
Purity
98.0
Solubility
DMSO : 100 mg/mL (ultrasonic)
Smiles
O=C(O)CCC1(CC2)CCC2(C(N3)=NC(N(CCC)C(N4CCC)=O)=C3C4=O)CC1
Molecular Formula
C22H32N4O4
Molecular Weight
416.51
References & Citations
[1]Kiesman WF, et al. Potent and orally bioavailable 8-bicyclo[2.2.2]octylxanthines as adenosine A1 receptor antagonists. J Med Chem. 2006 Nov 30;49 (24) :7119-31.|[2]Ensor CR, et al. Tonapofylline: a selective adenosine-1 receptor antagonist for the treatment of heart failure. Expert Opin Pharmacother. 2010 Oct;11 (14) :2405-15.|[3]Gill A, et al. Protective effect of tonapofylline (BG9928), an adenosine A1 receptor antagonist, against NSC 119875-induced acute kidney injury in rats. Am J Nephrol. 2009;30 (6) :521-6.
Shipping Conditions
Blue Ice
Storage Conditions
-20°C, 3 years (Powder)
Scientific Category
Reference compound1
Clinical Information
Phase 3
Available Sizes
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