LAS101057

LAS101057 is a potent adenosine A_2B receptor antagonist (K_i = 24 nM).¹ It is selective for A_2B over A_2A, 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 (NECA; Item No. 21420) in HEK293 cells expressing recombinant human A_2B 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.

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1. Eastwood, P., Esteve, C., Gonzalez, J., et al. Discovery of LAS101057: A potent, selective, and orally efficacious A2B adenosine receptor antagonist. Med. Chem. Lett. 2(3), 213-218 (2011).