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BAY-545 is an adenosine A2B receptor antagonist.1 It is selective for adenosine A2B receptors over A1, A2A, and A3 receptors with IC50 values of 66, 1,300, 820, and >6,700 nM, respectively, in CHO cell membranes expressing human recombinant receptors. BAY-545 reduces increases in the levels of IL-6 induced by the adenosine receptor agonist 5'-(N-ethylcarbamoyl)adenosine (NECA; Item No. 21420) in LL29 fibroblast cells (IC50 = 185 nM). It decreases FITC-induced increases in the levels of IL-6 in lung homogenates and cell numbers in bronchoalveolar lavage fluid (BALF) and reduces silica-induced increases in the levels of TGF-β1 in lung homogenates, but not cell numbers in BALF, in mouse models of pulmonary fibrosis when administered at a dose of 500 mg/kg.
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1. Novel non-