2. Signaling Pathways
  3. GPCR/G Protein
  4. Adenosine Receptor
  5. Adenosine A3 receptor (A3R) Isoform
  6. Adenosine A3 receptor (A3R) Antagonist

Adenosine A3 receptor (A3R) Antagonist

Adenosine A3 receptor (A3R) Antagonists (18):

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-153152
    DPTN dihydrochloride
    		Antagonist 98.66%
    DPTN is a potent and selective human, mouse, and rat A3AR antagonist with Ki values of 1.65, 9.61, and 8.53 nM, respectively.
  • 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-162787
    Adenosine receptor antagonist 5
    		Antagonist
    Adenosine receptor antagonist 5 (Compound 39) is a selective antagonist for human adenosine A3 receptor (hA3R) with Ki of 12 nM. Adenosine receptor antagonist 5 inhibits IB-MECA (HY-13591)-induced cAMP accumulation in NCI-H1792 cell, inhibits the proliferation of cancer cell LK-2 and NCI-H1792. Adenosine receptor antagonist 5 exhibits a fast metabolic rate in human liver microsomes.
  • HY-167905
    ATL444
    		Antagonist
    ATL444 is a adenosine receptor antagonist, with Ki values of 7.0, 2.5, 61.8, >1000 nM for rA1AR, rA2AAR, rA2BAR, rA3AR, respectively.
  • HY-103189
    VUF-5574
    		Antagonist 99.41%
    VUF-5574 is a selective antagonist of adenosine A3 receptor with a Ki of 4.03 nM for the recombinant human receptor.
  • HY-103176
    PSB11 hydrochloride
    		Antagonist
    PSB11 hydrochloride is an antagonist with reverse excitatory activity for human A3 Adenosine Receptor with high affinity (Ki=2.3 nM).
  • 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-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-146457
    A3AR antagonist 1
    		Antagonist
    A3AR antagonist 1 (compound 17) is a potent and selective human A3 adenosine receptor (AR) antagonist, with an Ki of 4.63 nM. A3AR antagonist 1 shows no affinity for the rat A3 AR even at high concentrations.
  • HY-12099
    A3AR antagonist 2
    		Antagonist
    A3AR antagonist 2 (compound 18) is a potent Human A3 adenosine receptor antagonist with an Ki value of 4.54 nM.
  • HY-147541
    A2A/A3 AR antagonist-1
    		Antagonist
    A2A/A3 AR antagonist-1 (compound 23) is a dual A2A/A3 adenosine receptor (AR) fluorescent ligand, with Kis of 90 nM and 31.8 nM for hA2A AR and hA3 AR, 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. A1/A3 AR antagonist 1 can be used for researching kidney failure, inflammatory pulmonary diseases, and Alzheimer’s disease.
  • HY-118086
    MRS1067
    		Antagonist
    MRS 1067 is a competitive antagonist of the adenosine A3 receptor that inhibits the suppression of adenylate cyclase by adenosine A3 receptor agonists and affects the activation of G proteins. MRS 1067 can be used in research related to inflammation and cancer.
  • 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.