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Submit ReviewAZ 1729 is a 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.
分子量 | 369.42 |
公式 | C18H16FN5OS |
储存 | Store at -20°C |
纯度 | ≥98% (HPLC) |
CAS Number | 2016864-46-1 |
InChI Key | HULFYSCAJVTAAR-UHFFFAOYSA-N |
Smiles | CC1=C(C2=CC(NC(C3=CC=C(C=C3)F)=O)=CC=C2)SC(NC(N)=N)=N1 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 36.94 | 100 | |
ethanol | 1.85 | 5 |
以下数据基于产品分子量 369.42。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 2.71 mL | 13.53 mL | 27.07 mL |
5 mM | 0.54 mL | 2.71 mL | 5.41 mL |
10 mM | 0.27 mL | 1.35 mL | 2.71 mL |
50 mM | 0.05 mL | 0.27 mL | 0.54 mL |
参考文献是支持产品生物活性的出版物。
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
If you know of a relevant reference for AZ 1729, please let us know.
关键词: AZ 1729, AZ 1729 supplier, AZ1729, free, fatty, acid, receptor, 2, biased, allosteric, agonists, agonism, functional, PAM, NAM, modulators, modulates, FFA2, GPCR, signaling, Free, Fatty, Acid, Receptors, 6826, Tocris Bioscience
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