| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| Other Sizes |
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| ln Vivo |
Tonapofylline (BG 9928) (1 mg/kg; po, bid, days 0-6) sustainably reduces post-NSC 119875 plasma muscle glucose and blood urea nitrogen levels, improves body weight, and restores significant NSC 119875-induced (5.5 mg/ kg)
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|---|---|
| Animal Protocol |
Animal/Disease Models: Female virus-free SD (SD (Sprague-Dawley)) rats [3]
Doses: 1 mg/kg Route of Administration: oral; renal pathology score [3]. twice (two times) daily, Days 0-6 Experimental Results: Serum creatinine and blood urea nitrogen levels were consistently diminished, weight recovery was improved, and NSC 119875-induced (5.5 mg/kg) renal pathology scores were Dramatically attenuated after NSC 119875. |
| 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.
[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. |
| Additional Infomation |
Tonapofylline is an oxopurine.
Tonapofylline has been used in trials studying the treatment of Heart Failure, Renal Insufficiency, and Congestive Heart Failure. Mechanism of Action Stimulation of A1 adenosine receptors in the kidney reduces glomerular filtration rate (GFR) via tubuloglomerular feedback and increases sodium reabsorption. Blocking A1 adenosine receptors would therefore maintain GFR and cause natriuresis. Tonapofylline is a xanthine derivative that binds with high affinity to A1 adenosine receptors from several species including human and acts as a competitive antagonist at these receptors. |
| Molecular Formula |
C22H32N4O4
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|---|---|
| Molecular Weight |
416.522
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| Exact Mass |
416.242
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| CAS # |
340021-17-2
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| PubChem CID |
216466
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| Appearance |
Typically exists as solid at room temperature
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| LogP |
3.163
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
30
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| Complexity |
687
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O([H])C(C([H])([H])C([H])([H])C12C([H])([H])C([H])([H])C(C3=NC4=C(C(N(C([H])([H])C([H])([H])C([H])([H])[H])C(N4C([H])([H])C([H])([H])C([H])([H])[H])=O)=O)N3[H])(C([H])([H])C1([H])[H])C([H])([H])C2([H])[H])=O
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| InChi Key |
ZWTVVWUOTJRXKM-UHFFFAOYSA-N
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| InChi Code |
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)
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| Chemical Name |
3-[4-(2,6-dioxo-1,3-dipropyl-7H-purin-8-yl)-1-bicyclo[2.2.2]octanyl]propanoic acid
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| Synonyms |
BG 9928; BG-9928; BG9928
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~240.09 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.00 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.00 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (4.99 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4008 mL | 12.0042 mL | 24.0085 mL | |
| 5 mM | 0.4802 mL | 2.4008 mL | 4.8017 mL | |
| 10 mM | 0.2401 mL | 1.2004 mL | 2.4008 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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