For research use only. Not for therapeutic Use.
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].
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].
| Catalog Number | I009676 |
| CAS Number | 340021-17-2 |
| Synonyms | 3-[4-(2,6-dioxo-1,3-dipropyl-7H-purin-8-yl)-1-bicyclo[2.2.2]octanyl]propanoic acid |
| Molecular Formula | C22H32N4O4 |
| Purity | ≥95% |
| InChI | InChI=1S/C22H32N4O4/c1-3-13-25-17-16(18(29)26(14-4-2)20(25)30)23-19(24-17)22-10-7-21(8-11-22,9-12-22)6-5-15(27)28/h3-14H2,1-2H3,(H,23,24)(H,27,28) |
| InChIKey | ZWTVVWUOTJRXKM-UHFFFAOYSA-N |
| SMILES | CCCN1C2=C(C(=O)N(C1=O)CCC)NC(=N2)C34CCC(CC3)(CC4)CCC(=O)O |
| Reference | [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. |
