Adenosine A2B receptor (A2BR) Antagonist
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PSB-1115
0 ImagesPSB-1115 is a selective A2B Adenosine Receptor antagonist. PSB-1115 inhibits the 2,4,6-trinitrobenzenesulfonic acid (TNBS)-induced contraction inhibition of acetylcholine (ACh).
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PSB36
0 ImagesPSB36 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.
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INCB106385
0 ImagesCat. No.: HY-184213CAS No.: 2408260-34-2INCB106385 is an orally active A2A/A2B adenosine receptor antagonist, with an IC50 value of 4.4 nM for cAMP inhibition at the A2A adenosine receptor and an IC50 value of 6.4 nM for cAMP inhibition at the A2B adenosine receptor. INCB106385 inhibits the pCREB signaling pathway in immune cells, blocks adenosine-mediated immunosuppression in the tumor microenvironment, and induces tumor regression. INCB106385 exhibits efficacy as a monotherapy or in combination with anti-PD-1 antibodies in colon cancer models. INCB106385 can be used for the research of colon cancer.
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MK-1088
0 ImagesCat. No.: HY-183599CAS No.: 2433765-51-4MK-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].
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M1069
0 ImagesM1069 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.
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8-(p-Sulfophenyl)theophylline
0 ImagesSynonyms: 8-SPT; 8-pSPT8-(p-Sulfophenyl)theophylline (8-SPT) (compound 2) is an adenosine A2B receptor antagonist, with a Ki of 1330 nM for A2B human recombinant.
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LAS38096
0 ImagesCat. No.: HY-111295CAS No.: 851371-22-7LAS38096 is a potent, selective, and efficacious A2B Adenosine Receptor antagonist, with a Ki of 17 nM.
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Adenosine receptor antagonist 7
0 ImagesCat. No.: HY-179248CAS No.: 2570904-69-5Adenosine 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.
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A2AAR antagonist 4
0 ImagesCat. No.: HY-175487CAS No.: 3114596-57-2A2AAR 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.
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ATL444
0 ImagesCat. No.: HY-167905CAS No.: 867054-13-5ATL444 is a adenosine receptor antagonist, with Ki values of 7.0, 2.5, 61.8, >1000 nM for rA1AR, rA2AAR, rA2BAR, rA3AR, respectively.
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Adenosine receptor antagonist 6
0 ImagesCat. No.: HY-175195CAS No.: 2913578-04-6Adenosine 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.
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SYAF080
0 ImagesCat. No.: HY-180424CAS No.: 352692-70-7SYAF080 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.
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A2AAR antagonist 5
0 ImagesCat. No.: HY-175851A2AAR 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.
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CVT-5440
0 ImagesCat. No.: HY-123038CAS No.: 531506-64-6
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CGH2466 dihydrochloride
0 ImagesCat. No.: HY-103167CAS No.: 1177618-54-0CGH 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).
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