Tonapofylline - CAS 340021-17-2
Catalog number: 340021-17-2
Category: Inhibitor
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Molecular Formula:
Molecular Weight:
Tonapofylline, a selective adenosine-1 receptor antagonist, has natriuretic effects and is able to maintain renal function, which can be beneficial to patients with congestive heart failure.
Solid powder
BG9928; BG-9928; BG 9928; Tonapofylline.3-(4-(2,6-dioxo-1,3-dipropyl-2,3,6,7-tetrahydro-1H-purin-8-yl)bicyclo[2.2.2]octan-1-yl)propanoic acid;
Soluble in DMSO
Store at -20 °C
Adenosine A1 receptor antagonists; Adenosine A2B receptor antagonists
Quality Standard:
Enterprise standard
Shelf Life:
As supplied, 2 years from the QC date provided on the Certificate of Analysis, when stored properly.
Canonical SMILES:
Current Developer:
CV Therapeutics
1.A1 adenosine receptor antagonists, agonists, and allosteric enhancers.
Kiesman WF1, Elzein E, Zablocki J. Handb Exp Pharmacol. 2009;(193):25-58. doi: 10.1007/978-3-540-89615-9_2.
Intense efforts of many pharmaceutical companies and academicians in the A(1) adenosine receptor (AR) field have led to the discovery of clinical candidates that are antagonists, agonists, and allosteric enhancers. The A(1)AR antagonists currently in clinical development are KW3902, BG9928, and SLV320. All three have high affinity for the human (h) A(1)AR subtype (hA(1) K (i) < 10 nM), > 200-fold selectivity over the hA(2A) subtype, and demonstrate renal protective effects in multiple animal models of disease and pharmacologic effects in human subjects. In the A(1)AR agonist area, clinical candidates have been discovered for the following conditions: atrial arrhythmias (tecadenoson, selodenoson and PJ-875); Type II diabetes and insulin sensitizing agents (GR79236, ARA, RPR-749, and CVT-3619); and angina (BAY 68-4986). The challenges associated with the development of any A(1)AR agonist are to obtain tissue-specific effects but avoid off-target tissue side effects and A(1)AR desensitization leading to tachyphylaxis.
2.Protective effect of tonapofylline (BG9928), an adenosine A1 receptor antagonist, against cisplatin-induced acute kidney injury in rats.
Gill A1, Wortham K, Costa D, Davis W, Ticho B, Whalley E. Am J Nephrol. 2009;30(6):521-6. doi: 10.1159/000248762. Epub 2009 Oct 13.
BACKGROUND/AIMS: Cisplatin (CIS) induces nephrotoxicity partly through renal vasoconstriction and decreased glomerular filtration effects thought to involve adenosine acting on adenosine A(1) receptors (A1Rs). We studied the effect of the orally active, A1R antagonist tonapofylline (BG9928) on biochemical measures of renal function in CIS-induced acute kidney injury (AKI) in rats.
3.Clinical pharmacokinetics of tonapofylline: evaluation of dose proportionality, oral bioavailability, and gender and food effects in healthy human subjects.
Li Z1, TenHoor C, Marbury T, Swan S, Ticho B, Rogge M, Nestorov I. J Clin Pharmacol. 2011 Jul;51(7):1004-14. doi: 10.1177/0091270010377633. Epub 2010 Oct 6.
Tonapofylline is an antagonist of adenosine A1 receptor being developed for heart failure. In the present studies, pharmacokinetic characteristics, including dose proportionality, bioavailability, and effects of gender and food, were evaluated in healthy subjects receiving single-dose tonapofylline (0.2-375 mg) in a parallel or crossover design. Following oral administration, tonapofylline concentrations mostly peaked within 3 hours and declined over time in a multiple phasic manner. Based on a power model, dose proportionality of peak concentration (C(max)), area under the time-concentration curve for all values (AUC(all)), and area under the time-concentration curve to infinity (AUC(inf)) was concluded in a clinical setting. The bioavailability of tonapofylline was 81.2% (90% confidence interval, 70.6%-93.5%). Following intravenous administration, the steady-state volume of distribution of tonapofylline was estimated to be 756 mL/kg. The total clearance of tonapofylline was low (64.
4.Pharmacokinetics and pharmacodynamics of tonapofylline in subjects with severe renal impairment and in elderly subjects.
Li Z1, Tenhoor C, Marbury T, Swan S, Zhu Y, Ticho B. Int J Clin Pharmacol Ther. 2011 Sep;49(9):563-70.
OBJECTIVE: The study was conducted to characterize the pharmacokinetics and pharmacodynamics of tonapofylline in subjects with severe renal impairment and in elderly subjects.
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CAS 340021-17-2 Tonapofylline

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