TUG-891

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.

Product information

CAS Number: 1374516-07-0

Molecular Weight: 364.41

Formula: C23H21FO3

Synonym:

TUG 891

TUG891

TUG-891

Chemical Name: 3-(4-((4-fluoro-4'-methyl-[1,1'-biphenyl]-2-yl)methoxy)phenyl)propanoic acid

Smiles: CC1C=CC(=CC=1)C1=CC=C(F)C=C1COC1C=CC(CCC(O)=O)=CC=1

InChiKey: LPGBXHWIQNZEJB-UHFFFAOYSA-N

InChi: InChI=1S/C23H21FO3/c1-16-2-7-18(8-3-16)22-12-9-20(24)14-19(22)15-27-21-10-4-17(5-11-21)6-13-23(25)26/h2-5,7-12,14H,6,13,15H2,1H3,(H,25,26)

Technical Data

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

In Vitro:

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.

References:

1. 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
2. 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.
3. 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.

Products are for research use only. Not for human use.