Adenosine Receptors

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  1. Reversine

    Catalog No. A13250
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    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. Learn More
  2. Pentostatin

    Catalog No. A11534
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    Adenosine deaminase inhibitor
    Pentostatin is an irreversible inhibitor of adenosine deaminase (Ki = 2.5 pM). Learn More
  3. MT-DADMe-ImmA

    Catalog No. A13651
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    human 5'-methylthioadenosine phosphorylase inhibitor
    MT-DADMe-ImmA is an inhibitor of human 5'-methylthioadenosine phosphorylase (MTAP) with a Ki of 90 pM. Learn More
  4. A2A receptor antagonist 1

    Catalog No. A12567
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    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. Learn More
  5. AB-MECA

    Catalog No. A12189
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    A3 adenosine receptor agonist
    AB-MECA is a high affinity A3 adenosine receptor agonist, has high affinity for recombinant A1 and A3 receptors. Learn More
  6. CGS 21680

    Catalog No. A11354
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    adenosine A2A receptor agonist
    CGS 21680 is a selective adenosine A2A receptor agonist, with a Ki of 27 nM. Learn More
  7. APNEA

    Catalog No. A20845
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    A3 adenosine receptor agonist
    APNEA (N6-[2-(4-Aminophenyl)ethyl]adenosine) is a potent, non-selective A3 adenosine receptor agonist. Learn More
  8. LAS101057

    Catalog No. A21203
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    A2B receptor antagonist
    LAS101057 is a potent, selective, and orally efficacious A2B receptor antagonist. Learn More
  9. Tonapofylline

    Catalog No. A21328
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    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. Learn More
  10. LUF6000

    Catalog No. A21532
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    A3 adenosine receptor allosteric modulator
    LUF6000 is an allosteric modulator of the human A3 adenosine receptor (AR). Learn More
  11. EHNA hydrochloride

    Catalog No. A21585
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    Adenosine deaminase inhibitor
    EHNA hydrochloride is a specific inhibitor of adenosine deaminase, prevents dAdo degradation and increases mitochondrial dATP levels in fibroblasts. Learn More
  12. Rolofylline

    Catalog No. A21649
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    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. Learn More
  13. Derenofylline

    Catalog No. A21990
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    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. Learn More
  14. MRS 1754

    Catalog No. A21998
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    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. Learn More
  15. N6-Cyclohexyladenosine

    Catalog No. A21008
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    A1 receptor agonist
    N6-Cyclohexyladenosine is a selective A1 receptor agonist (EC50 = 8.2 nM). Learn More
  16. MRS1177

    Catalog No. A16871
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    Adenosine A3 receptor antagonist
    MRS1177 is a potent and selective human Adenosine A3 receptor (hA3AR) antagonist, with a Ki of 0.3 nM. Learn More
  17. MRS1186

    Catalog No. A16870
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    Adenosine A3 receptor antagonist
    MRS1186 is a potent and selective human Adenosine A3 receptor (hA3AR) antagonist, with a Ki of 7.66 nM. Learn More
  18. AZD-4635 (HTL1071)

    Catalog No. A16820
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    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. Learn More
  19. NECA

    Catalog No. A16962
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    Adenosine receptor agonist
    NECA is a high-affinity adenosine receptor agonist (Ki values are 6.2, 14, and 20 nM for human A3, A1 and A2A receptors respectively; EC50 = 2.4 μM for human A2B). Learn More
  20. Theophylline-7-acetic acid

    Catalog No. A16822
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    Adenosine receptor antagonist
    Theophylline-7-acetic acid (Acefylline), acting as an adenosine receptor antagonist, is a stimulant drug of the xanthine chemical class. Learn More
  21. MRS1706

    Catalog No. A16868
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    adenosine A2B receptor agonist
    MRS1706 is a selective adenosine A2B receptor inverse agonist with Ki values of 1.39, 157, 112, and 230 nM for human A2B, A1, A2A, and A3 receptors, respectively. Learn More
  22. BAY-545

    Catalog No. A20116
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    A2B adenosine receptor antagonist
    BAY-545 is a potent and selective A2B adenosine receptor antagonist, with an IC50 of 59 nM. Learn More
  23. ST3932

    Catalog No. A12880
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    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. Learn More
  24. Tecadenoson

    Catalog No. A13302
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    A1 adenosine receptor agonist
    Tecadenoson (CVT-510) is a selective A1 adenosine receptor agonist. Learn More
  25. CPI-444

    Catalog No. A19242
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    A2AR antagonist
    CPI-444 is a potent, oral and selective A2A receptor (A2AR) antagonist, which induces antitumor responses. Learn More
  26. CGS-15943

    Catalog No. A14327
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    Adenosine A Receptor antagonist
    CGS 15943 is a potent, non-selective Adenosine A Receptor antagonist. It is orally active in vivo. Learn More
  27. SYN-115 (Tozadenant)

    Catalog No. A11560
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    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. Learn More
  28. CGS 21680 HCl Hydrate

    Catalog No. A11619
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    Adenosine A2A Receptor Agonist
    CGS 21680 is a specific adenosine A2A subtype receptor agonist. Learn More
  29. Adenosine

    Catalog No. A10040
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    Adenosine plays an important role in biochemical processes, such as energy transfer-as adenosine triphosphate (ATP) and adenosine diphosphate (ADP)-as well as in signal transduction as cyclic adenosine monophosphate, cAMP. It is also an inhibitory neurotransmitter. Learn More
  30. Aminophylline

    Catalog No. A10066
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    Adenosine receptor antagonist
    Aminophylline is a nonselective adenosine receptor antagonist and phosphodiesterase inhibitor capable of reversing ischemia-induced bradyasystole. Learn More
  31. Dyphylline

    Catalog No. A10339
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    Adenosine receptor antagonist
    Dyphylline is a xanthine derivative with bronchodilator and vasodilator effects. It acts as an adenosine receptor antagonist and phosphodiesterase inhibitor. Learn More
  32. SCH 442416

    Catalog No. A12695
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    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). Learn More
  33. Tamsulosin hydrochloride

    Catalog No. A12846
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    Tamsulosin hydrochloride is an antagonist of alpha1A adrenoceptors in the prostate. Learn More
  34. CVT 6883

    Catalog No. A13745
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    adenosine A2B receptors antagonist
    CVT-6883, a selective A2B adenosine antagonist, represents a novel potential approach to treating cardiopulmonary diseases. Learn More
  35. Capadenoson

    Catalog No. A14159
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    Adenosine Receptor agonist
    Capadenoson is a selective agonist of adenosine-A1 receptor. Learn More
  36. 5-Iodotubercidin

    Catalog No. A13948
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    Adenosine kinase inhibitor
    5-Iodotubercidin is a potent adenosine kinase inhibitor with IC50 of 26 nM. Learn More
  37. CF-102

    Catalog No. A14402
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    Adenosine A3 receptor agonist
    CF-102 is an orally bioavailable, synthetic, highly selective adenosine A3 receptor (A3AR) agonist with potential antineoplastic activity. Learn More
  38. Proxyphylline

    Catalog No. A16821
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    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). Learn More
  39. IB-MECA

    Catalog No. A14345
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    Adenosine A3-R agonist
    IB-MECA has been shown to act as a potent and selective Adenosine A3-R agonist with Ki values of 1.1, 54 and 56 nM for Adenosine A3-R, Adenosine A1-R and Adenosine A2A-R, respectively. Learn More
  40. ZM-241385

    Catalog No. A13517
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    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. Learn More
  41. Preladenant

    Catalog No. A13504
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    Adenosine A2A receptor antagonist
    Preladenant is a potent and selective antagonist at the adenosine A2A receptor. Learn More
  42. SCH58261

    Catalog No. A15886
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    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. Learn More
  43. DPCPX

    Catalog No. A16104
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    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. Learn More
  44. 2-Chloroadenosine (CADO)

    Catalog No. A16105
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    Adenosine A Receptor agonist
    2-Chloroadenosine is a metabolically stable analog of adenosine that behaves as an Adenosine A Receptor agonist (Ki values are 300, 80 and 1900 nM for Adenosine A1-R, Adenosine A2A-R and Adenosine A3-R, respectively). Learn More
  45. CGS 21680 HCl

    Catalog No. A16441
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    Adenosine A2 receptor agonist
    CGS 21680 HCl is an adenosine A2 receptor agonist with IC50 of 22 nM, exhibits 140-fold over A1 receptor. Learn More
  46. Regadenoson

    Catalog No. A12541
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    A2A adenosine agonist
    Regadenoson was selective agonist for the A2A adenosine receptor versus the A1, A2B, and A3 receptors in binding and functional studies. Regadenoson was also found to be a full and potent agonist to cause coronary vasodilation, a response that has a very large A2A receptor reserve? Learn More
  47. Vipadenant (BIIB-014)

    Catalog No. A13963
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    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. Learn More
  48. Istradefylline (KW-6002)

    Catalog No. A11451
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    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. Learn More

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