AZ 1729

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Cat.No. 6826 - AZ 1729 | C18H16FN5OS | CAS No. 2016864-46-1
Description: FFA2 allosteric agonist; displays bias for the Gi signaling pathway
Chemical Name: 4-Fluoro-N-[3-[2-[(aminoiminomethyl)amino]-4-methyl-5-thiazolyl]phenyl]benzamide
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews
Literature (1)

Biological Activity

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.

Technical Data

M. Wt 369.42
Formula C18H16FN5OS
Storage Store at -20°C
Purity ≥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

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 36.94 100
ethanol 1.85 5

Preparing Stock Solutions

The following data is based on the product molecular weight 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.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 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

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References

References are publications that support the biological activity of the product.

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


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