| Bioactivity | 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]. | |||||||||
| Target | Ki: 7.4 nM (Human adenosine A1 receptor) | |||||||||
| 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: | |||||||||
| Name | Tonapofylline | |||||||||
| CAS | 340021-17-2 | |||||||||
| Formula | C22H32N4O4 | |||||||||
| Molar Mass | 416.51 | |||||||||
| Appearance | Solid | |||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | |||||||||
| Storage |
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| 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. |
Tonapofylline
CAS: 340021-17-2 F: C22H32N4O4 W: 416.51
Tonapofylline (BG 9928) is an orally active and selective adenosine A1 receptor antagonist with aKi of 7.4 nM for human
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