A blood-brain barrier permeable xanthine derivative that acts as a highly selective antagonist of Adenosine A1 receptor (A1R; Ki = 3.9nM, 130nM, 1.0uM, 4.0uM for human A1, A2A, A2B, and A3 respectively). Exhibits about 1,000-fold higher affinity and a 30-fold greater selectivity for A1R when compared to theophylline. Shown to competitively antagonize the inhibition of adenylate cyclase activity via A1 adenosine receptors in rat fat cells and the stimulation of adenylate cyclase via A2 adenosine receptors in human platelets. Exhibits hypertensive properties.
Solubility:DMSO
Molecular Formula:C₁₆H₂₄N₄O₂
Primary Target:A1
Primary Target Ki:3.9nM
Molar Mass:304.4
Appearance:Supplied as a white solid.
Purity:≥99% (HPLC)
Storage and Stability:May be stored at 4°C. For long-term storage, aliquot and store at 4°C. Do not freeze. For maximum recovery of product, centrifuge the original vial prior to removing the cap. Further dilutions can be made in assay buffer.
Important Note:This product as supplied is intended for research use only, not for use in human, therapeutic or diagnostic applications without the expressed written authorization of United States Biological.
Toxicity and Hazards: All products should be handled by qualified personnel only, trained in laboratory procedures.
