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Tonapofylline

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].

Product Specifications

CAS Number

[340021-17-2]

Product Name Alternative

BG 9928

UNSPSC

12352005

Target

Adenosine Receptor

Type

Reference compound

Related Pathways

GPCR/G Protein

Applications

Neuroscience-Neuromodulation

Field of Research

Metabolic Disease; Cardiovascular Disease

Assay Protocol

https://www.medchemexpress.com/tonapofylline.html

Purity

98.0

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

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

Molecular Formula

C22H32N4O4

Molecular Weight

416.51

References & Citations

[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.

Shipping Conditions

Blue Ice

Storage Conditions

-20°C, 3 years (Powder)

Scientific Category

Reference compound1

Clinical Information

Phase 3

Available Sizes

Curated Selection

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