AZ 1729 |
カタログ番号GC50578 |
AZ 1729 は強力な遊離脂肪酸 2 受容体 (FFA2) 活性化因子であり、直接的なアロステリック アゴニストおよび正のアロステリック モジュレーターとして作用します。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2016864-46-1
Sample solution is provided at 25 µL, 10mM.
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.
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 |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
Average Rating: 5
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