LAS101057 is a potent adenosine A2B receptor antagonist (Ki = 24 nM).1 It is selective for A2B over A2A, A1, and A3 receptors, as well as a panel of 340 enzymes, receptors, channels, and transporters at 10 μM. LAS101057 inhibits cAMP signaling induced by 5’-N-ethylcarboxamidoadenosine in HEK293 cells expressing recombinant human A2B receptors (IC50 = 120 nM). It reduces NECA-induced release of IL-6 in human primary dermal fibroblasts. LAS101057 (10 mg/kg) prevents methacholine-induced airway hyperresponsiveness (AHR) and reduces bronchoalveolar lavage fluid (BALF) levels of IL-4 and IL-13 in an ovalbumin-sensitized mouse model of asthma.
1.Eastwood, P., Esteve, C., Gonzalez, J., et al.Discovery of LAS101057: A potent, selective, and orally efficacious A2B adenosine receptor antagonistMed. Chem. Lett.2(3)213-218(2011)