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LAS101057

Chemical Structure : LAS101057

CAS No.: 925676-48-8

LAS101057 (LAS 101057)

Catalog No.: PC-20638Not For Human Use, Lab Use Only.

LAS101057 (LAS 101057) is a potent, selective, and orally efficacious A2B adenosine receptor antagonist with Ki of 24 nM (human A2B).

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

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.

Physicochemical Properties

M.Wt 335.34
Formula C18H14FN5O
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

N-(5-(3-fluoropyridin-4-yl)-6-(pyridin-3-yl)pyrazin-2-yl)cyclopropanecarboxamide

References

1. Paul Eastwood, et al. ACS Med Chem Lett. 2011 Mar 10; 2(3): 213–218.

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