Tonapofylline
Based on 1 Customer Validation
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.
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- Purity: 98.99%
- CAS No.: 340021-17-2
- 화학식: C22H32N4O4
- 분자량:416.51
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보관:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
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Biological Activity
Ki: 7.4 nM (Human adenosine A1 receptor)[1]
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female viral antigen-free Sprague-Dawley rats[3]
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Dosage:1 mg/kg
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Administration:Oral administration; twice a day, days 0-6
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Result:Produced sustained reductions in post-NSC 119875 serum creatinine and blood urea nitrogen levels, improved body weight recovery and significant attenuation of NSC 119875-induced (5.5 mg/kg) kidney pathology scores.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 340021-17-2
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Appearance Solid
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분자량 416.51
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화학식 C22H32N4O4
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Color White to off-white
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SMILES
O=C(O)CCC1(CC2)CCC2(C(N3)=NC(N(CCC)C(N4CCC)=O)=C3C4=O)CC1
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Synonyms
BG 9928
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
DMSO : 100 mg/mL (240.09 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.00 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.00 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
순도&문서
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Data Sheet (273 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
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- Italian - IT (251 KB)
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- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.4009 mL | 12.0045 mL | 24.0090 mL | 60.0226 mL |
| 5 mM | 0.4802 mL | 2.4009 mL | 4.8018 mL | 12.0045 mL | |
| 10 mM | 0.2401 mL | 1.2005 mL | 2.4009 mL | 6.0023 mL | |
| 15 mM | 0.1601 mL | 0.8003 mL | 1.6006 mL | 4.0015 mL | |
| 20 mM | 0.1200 mL | 0.6002 mL | 1.2005 mL | 3.0011 mL | |
| 25 mM | 0.0960 mL | 0.4802 mL | 0.9604 mL | 2.4009 mL | |
| 30 mM | 0.0800 mL | 0.4002 mL | 0.8003 mL | 2.0008 mL | |
| 40 mM | 0.0600 mL | 0.3001 mL | 0.6002 mL | 1.5006 mL | |
| 50 mM | 0.0480 mL | 0.2401 mL | 0.4802 mL | 1.2005 mL | |
| 60 mM | 0.0400 mL | 0.2001 mL | 0.4002 mL | 1.0004 mL | |
| 80 mM | 0.0300 mL | 0.1501 mL | 0.3001 mL | 0.7503 mL | |
| 100 mM | 0.0240 mL | 0.1200 mL | 0.2401 mL | 0.6002 mL |
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