LAS101057 (LAS 101057) is a potent, selective, and orally efficacious A2B adenosine receptor antagonist with Ki of 24 nM (human A2B).
LAS101057 is >400-fold selective in a diverse panel of more than 340 enzymes, receptors, channels, and transporters.
LAS101057 effects a concentration-dependent down-regulation of IL-6 production with a potency (67%) at 100 nM on NECA-induced IL-6 release in human primary dermal fibroblasts.
LAS101057 (10 mg/kg) is active in an ovalbumin (OVA)-sensitized mouse model after oral administration, reducing airway hyperresponsiveness to methacholine, Th2 cytokine production, and OVA-specific IgE levels.
