For research use only. Not for therapeutic Use.
BAY 60-6583 is a potent and high-affinity agonist of adenosine A2B receptor (EC50 = 3 nM) over A1, A2A, and A3 receptors. BAY 60-6583 binds to mouse, rabbit, and dog A2BAR with Ki values of 750 nM, 340 nM and 330 nM, respectively. BAY 60-6583 has a cardioprotective effect in a myocardial ischemia model[1][5].
BAY 60-6583 exhibits? EC50 values for receptor activation >10,000 nM for both A1 and A2A AR and 3 nM for A2B AR subtype in CHO cells expressing recombinant human A1, A2A or A2B ARs[1].?
BAY 60-6583(0-10 μM) exhibits the maximum agonist effect of BAY in the absence of siRNA is 68 %, which is significantly different from that in the presence of 5, 50 and 500 nM siRNA (54%, 48% and 36%, respectively). It exhibits EC50 ?values of BAY in the absence and presence siRNA with 98±22, 102±17, 127±31 and 93±19 nM, respectively, in T24 cells[3].?
BAY 60-6583 (5 μM; 24 hours) increases the accumulation of cells at the G1 phase with a decrease in G2/M phase in RAW264.7 preosteoclasts[4].?
BAY 60-6583 (5 μM; 24 hours) specifically inhibits the activation of Akt by M-CSF, whereas M-CSF-induced ERK1/2 activation is not affected by BAY 60-6583 treatment in RAW264.7 preosteoclasts[4].
BAY 60-6583 (intravenous?injection; 100 mcg/kg) reduces the infarction area just prior to reperfusion in ischaemic rabbit hearts[1].?
BAY 60-6583 (intraperitoneal?injection; 2 mg/kg) attenuates LPS-induced lung injury, pre-treatment with this compound can significantly decrease LPS-increased? IL-6 levels in WT-mice, In contrast, BAY 60-6583 treatment is ineffective in abrogating these inflammatory parameters in ?A2BAR?/? ?mice[2].?
BAY 60-6583 (intratumoral administration) causes a significant increase in tumor-infiltrating MDSCs, it does not affect neither their ability to suppress T-cell proliferation nor their degree of maturation, it also stimulates the production of IL-10 and CCL2 in the tumor tissue[5].
| Catalog Number | I013985 |
| CAS Number | 910487-58-0 |
| Synonyms | 2-[6-amino-3,5-dicyano-4-[4-(cyclopropylmethoxy)phenyl]pyridin-2-yl]sulfanylacetamide |
| Molecular Formula | C19H17N5O2S |
| Purity | ≥95% |
| InChI | InChI=1S/C19H17N5O2S/c20-7-14-17(12-3-5-13(6-4-12)26-9-11-1-2-11)15(8-21)19(24-18(14)23)27-10-16(22)25/h3-6,11H,1-2,9-10H2,(H2,22,25)(H2,23,24) |
| InChIKey | ZTYHZMAZUWOXNC-UHFFFAOYSA-N |
| SMILES | C1CC1COC2=CC=C(C=C2)C3=C(C(=NC(=C3C#N)SCC(=O)N)N)C#N |
| Reference | [1]. Aherne CM, et al. Epithelial-specific A2B adenosine receptor signaling protects the colonic epithelial barrier during acute colitis.Mucosal Immunol. 2015 Nov;8(6):1324-38. [2]. Schingnitz U, et al. Signaling through the A2B adenosine receptor dampens endotoxin-induced acute lung injury.J Immunol. 2010 May 1;184(9):5271-9. [3]. Gao ZG, et al. Probing biased/partial agonism at the G protein-coupled A(2B) adenosine receptor.Biochem Pharmacol. 2014 Aug 1;90(3):297-306. [4]. Yoon Taek Oh, et al. A2B Adenosine Receptor Stimulation Down-regulates M-CSF-mediated Osteoclast Proliferation. Biomed Sci Letters 2017;23:194-200 [5]. John A. Auchampach, et al. Characterization of the A2B Adenosine Receptor from Mouse, Rabbit, and Dog. J Pharmacol Exp Ther. 2009 Apr;329(1):2-13. [6]. Morello S1, et al. Targeting the adenosine A2b receptor in the tumor microenvironment overcomes local immunosuppression by myeloid-derived suppressor cells.Oncoimmunology. 2014 Feb 14;3:e27989. eCollection 2014. |
