A potent adenosine A2B receptor antagonist (Ki = 24 nM); selective for A2B over A2A

LAS101057 – 5 mg

Brand:
Cayman
CAS:
925676-48-8
Storage:
-20
UN-No:
Non-Hazardous - /

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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SKU: 28435 - 5 mg Category:

Description

A potent adenosine A2B receptor antagonist (Ki = 24 nM); selective for A2B over A2A, A1, and A3 receptors, as well as a panel of 340 enzymes, receptors, channels, and transporters at 10 μM; inhibits NECA-induced cAMP signaling in HEK293 cells expressing recombinant human A2B receptors (IC50 = 120 nM); reduces NECA-induced release of IL-6 in human primary dermal fibroblasts; prevents methacholine-induced AHR and reduces BALF levels of IL-4 and IL-13 in an ovalbumin-sensitized mouse model of asthma

Formal name: N-[5-(3-fluoro-4-pyridinyl)-6-(3-pyridinyl)-2-pyrazinyl]-cyclopropanecarboxamide

Synonyms: 

Molecular weight: 335.3

CAS: 925676-48-8

Purity: ≥95%

Formulation: A solid

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