2. Signaling Pathways
  3. GPCR/G Protein
  4. Adenosine Receptor
  5. Adenosine A2B receptor (A2BR) Isoform
  6. Adenosine A2B receptor (A2BR) Antagonist

Adenosine A2B receptor (A2BR) Antagonist

Adenosine A2B receptor (A2BR) Antagonists (17):

Cat. No. Product Name Effect Purity
  • HY-103182
    PSB-1115
    		Antagonist 99.09%
    PSB-1115 is a selective A2B Adenosine Receptor antagonist. PSB-1115 inhibits the 2,4,6-trinitrobenzenesulfonic acid (TNBS)-induced contraction inhibition of acetylcholine (ACh).
  • HY-103175
    PSB36
    		Antagonist 99.94%
    PSB36 is a highly selective A1 adenosine receptor antagonist, with a Ki of 0.12 nM and a Kd of 0.7 nM. Systemic administration of PSB36 reduces formalin- and Carrageenan (HY-125474)-induced edema in mice and decreases pain-related behaviors, with no local paw activity. PSB36 prolongs the APD90 of rat and human atria, produces a frequency-dependent prolongation of rat atrial ERP, increases the diastolic threshold of rat atria, and shortens the duration of atrial fibrillation episodes. PSB36 can be used in research related to inflammatory pain, inflammatory hyperalgesia, edema and atrial fibrillation.
  • HY-129092
    8-(p-​Sulfophenyl)​theophylline
    		Antagonist ≥98.0%
    8-(p-Sulfophenyl)theophylline (8-SPT) (compound 2) is an adenosine A2B receptor antagonist, with a Ki of 1330 nM for A2B human recombinant.
  • HY-183599
    MK-1088
    		Antagonist
    MK-1088 is an orally active A2A/A2B adenosine receptor antagonist with human A2A Ki of 0.31 nM, human A2B Ki 5.3 nM. MK-1088 blocks receptor downstream signaling, inhibits CREB phosphorylation and reverses adenosine-mediated immunosuppression. MK-1088 restores TNF−α release and enhances tumor immune surveillance. MK-1088 can be used for the research of cancer[1].
  • HY-179671
    A3AR antagonist 6
    		Antagonist
    A3AR antagonist 6 (Compound 5p) is a selective A3AR antagonist with a Ki of 6.8 nM. A3AR antagonist 6 can be used in tumor research.
  • HY-148088
    M1069
    		Antagonist 99.52%
    M1069 is a selective and orall active, dual A2A/A2B adenosine receptor antagonist with a selectivity of >100 fold against the A1 and A3 receptors. M1069 counteracts immune-suppressive mechanisms of adenosine, and exhibits anti-tumor activity.
  • HY-148076
    A2A receptor antagonist 3
    		Antagonist 99.46%
    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-111295
    LAS38096
    		Antagonist
    LAS38096 is a potent, selective, and efficacious A2B Adenosine Receptor antagonist, with a Ki of 17 nM.
  • HY-179248
    Adenosine receptor antagonist 7
    		Antagonist
    Adenosine receptor antagonist 7 is an orally active triple A1/A2A/A2B adenosine receptor antagonist with Ki values of 1.5, 0.6 and 21 nM. Adenosine receptor antagonist 7 shows potent inhibitory activity (IC50 = 0.8 nM) of cAMP production in A2AR-HEK293 cells. Adenosine receptor antagonist 7 can enhance infiltration of effector T cells and increase the CD8+/Treg ratio companied with Avelumab (HY-108730). Adenosine receptor antagonist 7can be used for the research of cancer, such as colon cancer.
  • HY-175487
    A2AAR antagonist 4
    		Antagonist
    A2AAR antagonist 4 is an orally active A2A Adenosine receptor antagonist with a Ki of 0.36 nM and a KB of 1 nM at hA2AAR. A2AAR antagonist 4 fully inhibits hA2AAR and hA2bAR at 10 μM. A2AAR antagonist 4 can be used for research of cancer, such as MC38 tiumor.
  • 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-175195
    Adenosine receptor antagonist 6
    		Antagonist
    Adenosine receptor antagonist 6 is an orally active and selective A2A adenosine receptor (A2AAR) antagonist, with a Ki of 19.18 nM. Adenosine receptor antagonist 6 inhibits 5’-N-ethylcarboxamide adenosine (NECA) (HY-103173)-mediated cAMP production (IC50 = 0.089 μM) and immunosuppression, while promoting IL-2 and IFN-γ secretion. Adenosine receptor antagonist 6 abolishes the immunosuppressive effects of adenosine on T-cell activation and cytokine release. Adenosine receptor antagonist 6 inhibits tumor growth in a CT26/MC38 xenograft model. Adenosine receptor antagonist 6 can be used for the study of colon cancer.
  • HY-158057
    A2AR/A2BR antagonist 1
    		Antagonist
    A2AR/A2BR antagonist 1 (compound 7ai) has a dual antagonistic effect on A2AR/A2BR, with the IC50 values of 11.2 nM and 6.4 nM for A2AR and A2BR, respectively. A2AR/A2BR antagonist 1 promotes T cell-mediated cancer cell death.
  • HY-180424
    SYAF080
    		Antagonist
    SYAF080 is a human A₂B adenosine receptor (hA₂B AdoR) antagonist with a Ki of 23.6 nM and a KB of 25.2 nM. SYAF080no relevant inhibition of human CYP450 cytochromes. SYAF080 can be used for the research of inflammation, metabolic and cardiovascular disease.
  • HY-175851
    A2AAR antagonist 5
    		Antagonist
    A2AAR antagonist 5 is a selective A2AAR antagonist. A2AAR antagonist 5 inhibits NECA-stimulated adenylyl cyclase activity in hA2AAR-expressing CHO cells with an IC50 value of 1863 nM. A2AAR antagonist 5 possesses strong free radical scavenging activity, with an EC50 value of 22.21 μM in the DPPH assay. A2AAR antagonist 5 exerts notable neuroprotective effects in in vitro cerebral ischemia models. A2AAR antagonist 5 can be used for the study of cerebral ischemia.
  • 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-103167
    CGH2466 dihydrochloride
    		Antagonist
    CGH 2466 dihydrochloride is an orally active adenosine A1, A2B and A3 receptor antagonist with the IC50 values of 19 nM, 21 nM, and 80 nM respectively. CGH 2466 dihydrochloride inhibits p38 MAPK (IC50 = 187~ 400 nM) and phosphodiesterase type 4D (IC50 = 22 nM). CGH 2466 dihydrochloride displays potent anti-inflammatory effects both in vitro and in vivo, and can be used for research on asthma and chronic obstructive pulmonary disease (COPD).