A potent adenosine A2B receptor antagonist
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LAS101057

Item No. 28435

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[5-(3-fluoro-4-pyridinyl)-6-(3-pyridinyl)-2-pyrazinyl]-cyclopropanecarboxamide
CAS Number
925676-48-8
Molecular Formula
C18H14FN5O
Formula Weight
335.3
Purity
≥95%
Formulation (Request formulation change)
A solid
λmax
232, 281, 318 nm
SMILES
O=C(C1CC1)NC2=CN=C(C3=CC=NC=C3F)C(C4=CN=CC=C4)=N2
InChi Code
InChI=1S/C18H14FN5O/c19-14-9-21-7-5-13(14)17-16(12-2-1-6-20-8-12)23-15(10-22-17)24-18(25)11-3-4-11/h1-2,5-11H,3-4H2,(H,23,24,25)
InChi Key
XUYURJQIMYCWBB-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $69

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    10 mg

    $120

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    25 mg

    $280

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    50 mg

    $525

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    Product Description

    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 (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.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    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).