BAY-545

BAY-545 is an adenosine A2B receptor antagonist. 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, Cay-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-beta1 in lung homogenates, but not cell numbers in BALF, in mouse models of pulmonary fibrosis when administered at a dose of 500 mg/kg.Formal Name: 3-ethyl-6-[(4-hydroxy-1-piperidinyl)carbonyl]-5-methyl-1-(3,3,3-trifluoropropyl)-thieno[2,3-d]pyrimidine-2,4(1H,3H)-dione. CAS Number: 1699717-32-2. Molecular Formula: C18H22F3N3O4S. Formula Weight: 433.4. Purity: >95%. Formulation: (Request formulation change), A solid. Solubility: DMSO: 150 mg/ml. lambdamax: 231, 286 nm. SMILES: O=C1N(CC)C(C2=C(SC(C(N3CCC(O)CC3)=O)=C2C)N1CCC(F)(F)F)=O. InChi Code: InChI=1S/C18H22F3N3O4S/c1-3-23-14(26)12-10(2)13(15(27)22-7-4-11(25)5-8-22)29-16(12)24(17(23)28)9-6-18(19,20)21/h11,25H,3-9H2,1-2H3. InChi Key: NTYVAKNEYLJAPT-UHFFFAOYSA-N.