Adenosine Receptors

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  1. Adenosine receptor antagonist

    Aminophylline is a nonselective adenosine receptor antagonist and phosphodiesterase inhibitor capable of reversing ischemia-induced bradyasystole.
  2. Adenosine receptor antagonist

    Dyphylline is a xanthine derivative with bronchodilator and vasodilator effects. It acts as an adenosine receptor antagonist and phosphodiesterase inhibitor.
  3. A2A antagonist

    Istradefylline (KW-6002) is a selective antagonist at the A2A receptor. It has been found to be useful in the treatment of Parkinson's disease.
  4. A2a receptor antagonist

    SYN115 is an orally administered, potent and selective inhibitor of the adenosine 2a (A2a) receptor that is being developed initially for the treatment of Parkinson?€?s disease, but may also have utility in other CNS disorders.
  5. adenosine A2A/A1 receptor antagonist

    A2A receptor antagonist 1 (CPI-444 analog) is an antagonist of both adenosine A2A receptor and A1 receptor with Kis of 4 and 264 nM, respectively.
  6. A2A Receptor Antagonist

    SCH 442416 is a selective adenosine A2A receptor antagonist; binds to human and rat A2A receptors with high affinity (Ki values are 0.048 and 0.5 nM respectively). Displays > 23000-fold selectivity for hA2A over hA1 in vitro with minimal affinity for hA2B and hA3 receptors (IC50 > 10 μM).
  7. Adenosine A2A receptor antagonist

    ST3932 is a metabolite of ST1535, acts as an antagonist of adenosine A2A receptor, with Kis of 8 nM and 33 nM for A2A and A1 receptors, respectively.
  8. human A3 adenosine receptor antagonist /Aurora inhibitor

    Reversine is a potent human A3 adenosine receptor antagonist with Ki of 0.66 μM, and a pan-aurora A/B/C kinase inhibitor with IC50 of 12 nM/13 nM/20 nM, respectively. Also used for stem cell dedifferentiation.
  9. Adenosine A2A receptor antagonist

    Preladenant is a potent and selective antagonist at the adenosine A2A receptor.
  10. Adenosine A2A antagonist

    ZM-241385 is a potent and highly selective Adenosine A2A-R antagonist, with a pA2 of 9.02 for Adenosine A2A-R in cardiac vasculature and selectivities of 1000, 91 and 500,000 over Adenosine A1-R, Adenosine A2B-R and Adenosine A3-R sites, respectively.
  11. adenosine A2B receptors antagonist

    CVT-6883, a selective A2B adenosine antagonist, represents a novel potential approach to treating cardiopulmonary diseases.
  12. A2A receptor antagonist

    Vipadenant, also known as BIIB014, CEB-4520, is a potent, selective and orally available adenosine A2A receptor antagonist under development for Parkinson's disease. Vipadenant demonstrates strong oral activity in commonly used models of Parkinson's disease.
  13. Adenosine A Receptor antagonist

    CGS 15943 is a potent, non-selective Adenosine A Receptor antagonist. It is orally active in vivo.
  14. Adenosine A3 receptor agonist

    CF-102 is an orally bioavailable, synthetic, highly selective adenosine A3 receptor (A3AR) agonist with potential antineoplastic activity.
  15. A2A adenosine receptor antagonist

    SCH58261 is a potent and selective A2a adenosine receptor antagonist with Ki of 2.3 nM and 2 nM for rat A2a and bovine A2a, respectively.
  16. Adenosine A1-R antagonist

    DPCPX, a xanthine derivative, is a very potent and selective Adenosine A1-R antagonist. It displays very modest efficacy against Adenosine A2A-R, Adenosine A2B-R and Adenosine A3-R.
  17. A2 receptor antagonist

    Alloxazine is an A2 receptor antagonist, which is approximately 10-fold more selective for the A2B receptor than for the A2A receptor.
  18. A2AR antagonist

    AZD-4635 (HTL1071) is an oral A2AR antagonist that binds to human A2AR with a Ki of 1.7 nM and with > 30-fold selectivity over other adenosine receptors.
  19. A1 adenosine receptors antagonist

    Proxyphylline is a derivative of theophylline which is used as a bronchodilator and for its cardiovascular properties. It selectively antagonizes A1 adenosine receptors (Ki = 82 nM for bovine brain) versus A2 adenosine receptors (Ki = 850 μM for platelets).
  20. Adenosine receptor antagonist

    Theophylline-7-acetic acid (Acefylline), acting as an adenosine receptor antagonist, is a stimulant drug of the xanthine chemical class.
  21. Adenosine A3 receptor antagonist

    MRS1186 is a potent and selective human Adenosine A3 receptor (hA3AR) antagonist, with a Ki of 7.66 nM.
  22. Adenosine A3 receptor antagonist

    MRS1177 is a potent and selective human Adenosine A3 receptor (hA3AR) antagonist, with a Ki of 0.3 nM.
  23. adenosine A3 receptor antagonist

    MRE3008F20 is a highly potent and selective antagonist of adenosine A3 receptor (AA3R), inhibits agonist-induced cAMP elevation in resting T lymphocytes with an IC50 of 5 nM.
  24. A2B adenosine receptor antagonist

    BAY-545 is a potent and selective A2B adenosine receptor antagonist, with an IC50 of 59 nM.
  25. adenosine receptor antagonist

    Taminadenant is an antagonist of adenosine receptor.
  26. AA3R antagonist

    Adenosine antagonist-1 is an adenosine A3 receptor (AA3R) antagonist.
  27. A2B receptor antagonist

    LAS101057 is a potent, selective, and orally efficacious A2B receptor antagonist.
  28. adenosine A1 receptor antagonist

    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.
  29. adenosine A1 receptor antagonist

    Rolofylline (KW-3902) is a potent, selective adenosine A1 receptor antagonist that is under development for the treatment of patients with acute congestive heart failure and renal impairment.
  30. adenosine A1 receptor antagonist

    Derenofylline (SLV 320) is a potent, selective and orally active adenosine A1 receptor antagonist, with Ki values of 1 nM, 200 nM and 398 nM for human A1, A3 and A2A receptors respectively.
  31. A2B adenosine receptor antagonist

    MRS 1754 is a selective antagonist radioligand for A2B adenosine receptor with very low affinity for A1 and A3 receptors of both humans and rats.
  32. adenosine receptor antagonist

    AB928 is an orally bioavailable, selective dual adenosine receptor (A2aR/A2bR) antagonist. AB928 relieves adenosine-mediated immune suppression. AB928 has immunomodulatory and antitumor activities.

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