Formulation: A solid
Formal Name: N-[5-(3-fluoro-4-pyridinyl)-6-(3-pyridinyl)-2-pyrazinyl]-cyclopropanecarboxamide
Purity: ≥95%
Formula Markup: C18H14FN5O
Formula Weight: 335,3
Shelf life (days): 1460
CAS Number: 925676-48-8
Notes: LAS101057 is a potent adenosine A2B receptor antagonist (Ki = 24 nM).{50134} 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 (NECA; Item No. 21420) 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.
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