1. Signaling Pathways
  2. GPCR/G Protein
  3. Adenosine Receptor
  4. Adenosine A1 receptor (A1R) Isoform
  5. Adenosine A1 receptor (A1R) Antagonist

Adenosine A1 receptor (A1R) Antagonist

Adenosine A1 receptor (A1R) Antagonists (10):

Cat. No. Product Name Effect Purity
  • HY-14858
    Derenofylline
    Antagonist ≥99.0%
    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.
  • HY-147544
    A1AR antagonist 5
    Antagonist
    A1AR antagonist 5 (compound 20) is a potent and selective A1AR (A1 adenosine receptor) antagonist, with a pIC50 of 5.83 and a pKi of 6.11.
  • HY-148076
    A2A receptor antagonist 3
    Antagonist
    A2A receptor antagonist 3 (Example 92) is an adenosine A2a receptor antagonist with a Ki of 0.4 nM.
  • HY-147543
    A1AR antagonist 4
    Antagonist
    A1AR antagonist 4 (compound 22) is a potent and selective A1AR (A1 adenosine receptor) antagonist, with a pIC50 of 5.51 and a pKi of 6.29.
  • HY-103174
    MRS1334
    Antagonist
    MRS1334 is a potent and selective human adenosine A3 receptor antagonist with Kis of 2.69 nM, >100 nM, >100 nM for hA3, rA1, rA2A, respectively.
  • HY-147545
    A1AR antagonist 6
    Antagonist
    A1AR antagonist 6 (compound 15) is a potent and selective A1AR (A1 adenosine receptor) antagonist, with a pIC50 of 6.38 and a pKi of 7.13.
  • HY-146979
    hA2A/hCA XII modulator 1
    Antagonist
    hA2A/hCA XII modulator 1 (compound 14), a triazolopirazine, is a potent hA2A adenosine receptor (hA2AAR) antagonist with Kis of 6.4 nM, 4.819 μM, >30 μM for hA2AAR, hA1AR, hA3AR, respectively.
  • HY-103175
    PSB36
    Antagonist
    PSB36 is a potent and selective antagonist of adenosine A1 receptor, with Kis 0.12 nM, 187 nM, 552 nM, 2300 nM, and 6500 nM for rA1, hA2B, rA2A, hA3 and rA3 receptors respectively.
  • HY-146456
    A1AR antagonist 3
    Antagonist
    A1AR antagonist 3 (compound 13) is a selective adenosine 1 (A1) receptor antagonist with Kis of 9.69 nM and 0.529 nM for human A1 and rat A1, respectively.
  • HY-146478
    A1/A3 AR antagonist 1
    Antagonist
    A1/A3 AR antagonist 1 (compound 10) is a potent adenosine 1 (A1) and adenosine 3 (A3) receptor dual antagonist with Kis of 36.7 nM, 25.4 nM and 1.47 nM for human A1, human A3 and rat A1, respectively.