| Identification | Back Directory | [Name]
BG 9928 | [CAS]
340021-17-2 | [Synonyms]
BG 9928
Tonapofylline
ZWTVVWUOTJRXKM-UHFFFAOYSA-N
Bicyclo[2.2.2]octane-1-propanoic acid, 4-(2,3,6,7-tetrahydro-2,6-dioxo-1,3-dipropyl-1H-purin-8-yl)- | [Molecular Formula]
C22H32N4O4 | [MDL Number]
MFCD09970392 | [MOL File]
340021-17-2.mol | [Molecular Weight]
416.51 |
| Chemical Properties | Back Directory | [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 |
| Hazard Information | Back Directory | [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. |
| [storage]
Store at -20°C | [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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