ChemicalBook Product Catalog API Circulatory system drugs Anti-Congestive Heart Failure drugs BG 9928

BG 9928

Product NameBG 9928
CAS340021-17-2
MFC22H32N4O4
MW416.51
EINECS
MOL File340021-17-2.mol

Chemical Properties

Boiling point	665.3±51.0 °C(Predicted)
Density	1.273±0.06 g/cm3(Predicted)
storage temp.	Store at -20°C
solubility	Soluble in DMSO
form	Solid
pka	4.81±0.10(Predicted)
color	White to off-white

Usage And Synthesis

Uses

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].

Definition

ChEBI: Tonapofylline is an oxopurine.

in vivo

Tonapofylline (BG 9928) (1 mg/kg; p.o., b.i.d, days 0-6) produces sustained reductions in post-NSC 119875 serum creatinine and blood urea nitrogen levels, improves body weight recovery and significant attenuation of NSC 119875-induced (5.5 mg/kg) kidney pathology scores^[3].

Animal Model:	Female viral antigen-free Sprague-Dawley rats^[3]
Dosage:	1 mg/kg
Administration:	Oral administration; twice a day, days 0-6
Result:	Produced sustained reductions in post-NSC 119875 serum creatinine and blood urea nitrogen levels, improved body weight recovery and significant attenuation of NSC 119875-induced (5.5 mg/kg) kidney pathology scores.

References

[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. DOI:10.1021/jm0605381
[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. DOI:10.1517/14656566.2010.514605
[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. DOI:10.1159/000248762

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