Tonapofylline (Synonyms: BG 9928) |
| Catalog No.GC37815 |
토나포필린(BG 9928)은 인간 아데노신 A1 수용체(hA1)에 대해 7.4 nM의 Ki를 갖는 경구 활성 및 선택적 아데노신 A1 수용체 길항제이며, 이는 인간 아데노신 A2A 수용체에 대해 915배 선택성을 나타내고 인간 아데노신 A2B에 대해 12배 선택성을 나타냅니다. 수용체이며 심부전 치료를 위한 개발에 사용됩니다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 340021-17-2
Sample solution is provided at 25 µL, 10mM.
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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]. Ki: 7.4 nM (Human adenosine A1 receptor)[1]
Tonapofylline (BG 9928) (1 mg/kg; p.o., b.i.d, days 0-6) produces sustained reductions in post-Cisplatin serum creatinine and blood urea nitrogen levels, improves body weight recovery and significant attenuation of Cisplatin-induced (5.5 mg/kg) kidney pathology scores[3]. Animal Model: Female viral antigen-free Sprague-Dawley rats[3]
[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 cisplatin-induced acute kidney injury in rats. Am J Nephrol. 2009;30(6):521-6.
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