Adenosine Receptors

Adenosine receptor agonists and antagonists target A1, A2A, A2B and A3, the four G protein-coupled adenosine receptors. The International Union of Pharmacology (IUPHAR) set out this nomenclature in 2001. A1 and A3 receptors usually inhibit adenylyl cyclase, while A2A and A2B receptors stimulate it. In 2008 the human A2A receptor was crystallized bound to an antagonist at 2.6 Å resolution. Ligands in this category include the A2A agonist CGS 21680 HCl Hydrate, the A2A antagonist istradefylline and the A3 agonist IB-MECA. Xanthines such as theophylline block several subtypes, and 5-Iodotubercidin inhibits adenosine kinase, which phosphorylates adenosine.

3 Items

  • GS-9667
    Cat. No.
    A57898

    GS-9667

    Synonyms: CVT 3619

    GS-9667 is a selective partial agonist of the A1 adenosine receptor (A1AdoR). This N6-5'-substituted adenosine analog effectively reduces cyclic AMP levels and inhibits the release of nonesterified fatty acids from epididymal adipocytes, demonstrating IC50 values of 6 nM and 44 nM, respectively. Its ability to inhibit lipolysis suggests potential applications in research related to Type 2 diabetes (T2DM) and dyslipidemia by lowering free fatty acids (FFA).

    1 mg
    $55.00
    5 mg
    $140.00
    All 7 sizes
  • LUF5834
    Cat. No.
    A57917

    LUF5834

    LUF5834 is a selective partial agonist of the A2B adenosine receptor (A2BR), with an EC50 of 12 nM. Additionally, LUF5834 exhibits partial agonistic activity at the A1 and A2A adenosine receptors, with Ki values of 2.6 nM and 28 nM, respectively. This compound is valuable in studies investigating adenosine signaling pathways, receptor pharmacology, and potential therapeutic applications related to the modulation of adenosine receptor activity.

    5 mg
    $225.00
    25 mg
    $1,275.00
    All 4 sizes
  • CVT-2759 analog
    Cat. No.
    A58047

    CVT-2759 analog

    CVT-2759 analog is a partial agonist of the A1 adenosine receptor, exhibiting a Ki value of 167 nM. This compound is valuable for research into cardiac arrhythmias, providing insights into the modulation of adenosine receptor signaling and its implications in cardiac health. Its specificity for the A1 receptor makes it a suitable tool for studying the physiological effects of adenosine in cardiac tissue.

    25 mg
    $1,275.00
    50 mg
    $1,625.00
    All 3 sizes

3 Items

Added to your cart

View Cart Checkout

    Loading...