An adenosine A2B receptor antagonist
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BAY-545

Item No. 28420

Technical Information
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
Purity
≥95%
A solid
DMSO: 150 mg/ml
λmax
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
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    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.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Harter, M., Kalthof, B., Delbeck, M., et al. Novel non-xanthine antagonist of the A2B adenosine receptor: From HTS hit to lead structure. Eur. J. Med. Chem. 163, 763-778 (2019).