TUG-891 is a potent and selective agonist of the free fatty acid receptor 4 (FFA4/GPR120), which demonstrates both potential opportunity and possible challenges to therapeutic agonism. Activation of human FFA4 by TUG-891 also resulted in rapid phosphorylation and internalization of the receptor. TUG-891 was also a potent agonist of mouse FFA4, but it showed only limited selectivity over mouse FFA1, complicating its use in vivo in this species.
CAS Number: 1374516-07-0
Molecular Weight: 364.41
Chemical Name: 3-(4-((4-fluoro-4'-methyl-[1,1'-biphenyl]-2-yl)methoxy)phenyl)propanoic acid
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : ≥ 180 mg/mL (493.95 mM)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined.
HS Tariff Code: 382200
How to use
TUG-891 displays similar signaling properties to the LCFA α-linolenic acid at human FFA4, including stimulation of Ca2+ mobilization, β-arrestin-1 and β-arrestin-2 recruitment, and extracellular signal-regulated kinase phosphorylation. Activation of human FFA4 by TUG-891 also results in rapid phosphorylation and internalization of the receptor.
- Hudson BD, et al. The pharmacology of TUG-891, a potent and selective agonist of the free fatty acid receptor 4 (FFA4/GPR120), demonstrates both potential opportunity and possible challenges to therapeutic agonism. Mol Pharmacol. 2013 Nov;84(5):710-25
- Anbazhagan AN, Priyamvada S, Gujral T, Bhattacharyya S, Alrefai WA, Dudeja PK, Borthakur A. A Novel Anti-inflammatory Role of GPR120 in Intestinal Epithelial Cells. Am J Physiol Cell Physiol. 2016 Jan 20:ajpcell.00123.2015. doi: 10.1152/ajpcell.00123.2015. [Epub ahead of print] PubMed PMID: 26791484.
- Song T, Peng J, Ren J, Wei HK, Peng J. Cloning and characterization of spliced variants of the porcine G protein coupled receptor 120. Biomed Res Int. 2015;2015:813816. doi: 10.1155/2015/813816. Epub 2015 May 17. PubMed PMID: 26075265; PubMed Central PMCID: PMC4449883.
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