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

Adenosine A1 receptor (A1R) Antagonist

Adenosine A1 receptor (A1R) Antagonists (15):

Cat. No. Product Name Effect Purity
  • HY-14858
    Derenofylline
    		Antagonist 99.87%
    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. Derenofylline suppresses cardiac fibrosis and attenuates albuminuria without affecting blood pressure in rats.
  • HY-103175
    PSB36
    		Antagonist ≥99.0%
    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. PSB36 can be used for the research of hyperalgesia.
  • HY-103174
    MRS1334
    		Antagonist ≥99.0%
    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. MRS1334 blocks the protective effect of Cl-IB-MECA leading to significant bradycardia and elevated ST segment. MRS1334 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
  • HY-116800
    FR194921
    		Antagonist 98.10%
    FR194921 is a potent, selective and orally active and cross the blood-brain barrier Adenosine A1 antagonist with Ki value of 6.6, 5400 nM for A1, A2A, respectively. FR194921 shows cognitive-enhancing and anxiolytic activity.
  • 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-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-111295
    LAS38096
    		Antagonist
    LAS38096 is a potent, selective, and efficacious A2B Adenosine Receptor antagonist, with a Ki of 17 nM.
  • HY-120652
    A3AR antagonist 3
    		Antagonist
    A3AR antagonist 3 (compound 21) is a selective A3 adenosine receptor (A3AR) antagonist with a Ki of 37 nM. A3AR antagonist 3 shows >60-fold selectivity in comparison to A1 and A2A adenosine receptors.
  • 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-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. A2A receptor antagonist 3 also binds to A2b, A1 and A3 receptor with Kis of 37, 107 and 1467 nM, respectively.
  • 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. hA2A/hCA XII modulator 1 is a potent human carbonic anhydrase XII (hCA XII) inhibitor with Kis of 6.2 nM, 46 nM, 466 nM, 8.351 μM for hCA XII, hCA II, hCA IX and hCA I, respectively. hA2A/hCA XII modulator 1 has the potential for cancer research.
  • 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. A1AR antagonist 3 can be used for researching neurological diseases.
  • 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. A1/A3 AR antagonist 1 can be used for researching kidney failure, inflammatory pulmonary diseases, and Alzheimer’s disease.
  • HY-123038
    CVT-5440
    		Antagonist
    CVT-5440 is a xanthine based, selective, high affinity A2B adenosine receptors (AdoR) antagonist with a Ki of 50 nM (selectivity A1> 200; A2A>200; A3>167). CVT-5440 has the potential for asthma research.
  • HY-118232
    VUF8504
    		Antagonist
    VUF-8504 is a potent and selective adenosine A3 receptor antagonist with Ki value of 0.017, 14 nM for human A3, A1, respectively.