1. GPCR/G Protein
  2. Adenosine Receptor
  3. Tonapofylline

Tonapofylline (Synonyms: BG 9928)

Cat. No.: HY-14873 Purity: ≥98.0%
Handling Instructions

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.

For research use only. We do not sell to patients.

Tonapofylline Chemical Structure

Tonapofylline Chemical Structure

CAS No. : 340021-17-2

Size Price Stock Quantity
5 mg USD 250 In-stock
Estimated Time of Arrival: December 31
10 mg USD 380 In-stock
Estimated Time of Arrival: December 31
50 mg   Get quote  
100 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

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Description

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].

IC50 & Target

Ki: 7.4 nM (Human adenosine A1 receptor)[1]

In Vivo

Tonapofylline (BG 9928) (1 mg/kg; p.o., b.i.d, days 0-6) produces sustained reductions in post-NSC 119875 serum creatinine and blood urea nitrogen levels, improves body weight recovery and significant attenuation of NSC 119875-induced (5.5 mg/kg) kidney pathology scores[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female viral antigen-free Sprague-Dawley rats[3]
Dosage: 1 mg/kg
Administration: Oral administration; twice a day, days 0-6
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.
Clinical Trial
Molecular Weight

416.51

Formula

C₂₂H₃₂N₄O₄

CAS No.
SMILES

O=C(O)CCC1(CC2)CCC2(C(N3)=NC(N(CCC)C(N4CCC)=O)=C3C4=O)CC1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (240.09 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4009 mL 12.0045 mL 24.0090 mL
5 mM 0.4802 mL 2.4009 mL 4.8018 mL
10 mM 0.2401 mL 1.2005 mL 2.4009 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    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

  • 2.

    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

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (6.00 mM); Clear solution

*All of the co-solvents are provided by MCE.
References

Purity: ≥98.0%

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Keywords:

TonapofyllineBG 9928BG9928BG-9928Adenosine ReceptorP1 receptorInhibitorinhibitorinhibit

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Product Name:
Tonapofylline
Cat. No.:
HY-14873
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