AZ 1729

TargetMol
Product Code: TAR-T37896
Supplier: TargetMol
CodeSizePrice
TAR-T37896-50mg50mg£999.00
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Overview

Regulatory Status: RUO
Shipping:
cool pack
Storage:
-20℃

Images

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Further Information

Bioactivity:
FFA2 allosteric agonist. Inhibits forskolin-induced cAMP increase and stimulates 35SGTPγS binding in biochemical assays (pEC50 values are 6.9 and 7.23, respectively). Binds at allosteric binding site. In functional assays, displays positive allosteric modulation of FFA-induced Gi signaling and negative allosteric modulation of FFA-induced Gq/G11 signaling. Inhibits lipolytic effect of isoproterenol (pEC50 = 5.03) and induces migration of human neutrophils in vitro.
CAS:
2016864-46-1
Formula:
C18H16FN5OS
Molecular Weight:
369.42
Purity:
0.98
SMILES:
CC1=C(C2=CC(NC(C3=CC=C(C=C3)F)=O)=CC=C2)SC(NC(N)=N)=N1

References

Sergeev et al (2017) A single extracellular amino acid in free fatty acid receptor 2 defines antagonist species selectivity and G protein selection bias. Sci.Rep. 7 13741 PMID:29061999 Bolognini et al (2016) A novel allosteric activator of free fatty acid 2 receptor displays unique Gi-functional bias. J.Biol.Chem. 291 18915 PMID:27385588