Tonapofylline (Synonyms: BG 9928) |
Catalog No.GC37815
One-Click Copy Product Info
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La tonapofilina (BG 9928) es un antagonista del receptor de adenosina A1 selectivo y activo por vÍa oral con una Ki de 7,4 nM para el receptor de adenosina A1 humana (hA1), que muestra una selectividad de 915 veces frente al receptor de adenosina A2A humana y una selectividad de 12 veces frente a la adenosina A2B humana receptor y se utiliza en desarrollo para el tratamiento de la insuficiencia cardÍaca.
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.
| Cas No. | 340021-17-2 | SDF | |
| Sinónimos | BG 9928 | ||
| Canonical SMILES | O=C(O)CCC1(CC2)CCC2(C(N3)=NC(N(CCC)C(N4CCC)=O)=C3C4=O)CC1 | ||
| Formula | C22H32N4O4 | M.Wt | 416.51 |
| Solubility | DMSO : 100 mg/mL (240.09 mM; Need ultrasonic) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.4009 mL | 12.0045 mL | 24.009 mL |
| 5 mM | 480.2 μL | 2.4009 mL | 4.8018 mL |
| 10 mM | 240.1 μL | 1.2005 mL | 2.4009 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >96.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 6 reference(s) in Google Scholar.)