| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| Other Sizes |
Purity: ≥98%
| Targets |
FFA4/GPR120
Free fatty acid receptor 4 (FFA4/GPR120). TUG-891 is a potent and selective agonist that activates this receptor. Activation of FFA4 leads to a variety of downstream effects, including the promotion of Ca²⁺ mobilization, recruitment of β-arrestin-1 and β-arrestin-2, and phosphorylation of extracellular signal-regulated kinase. The compound is a valuable tool for studying the role of FFA4 in metabolism and inflammation. |
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| ln Vitro |
TUG-891 exhibits comparable signaling characteristics to the LCFA α-linolenic acid at human FFA4 at multiple assay end points, such as promoting Ca2+ mobilization, recruiting β-arrestin-1 and β-arrestin-2, and phosphorylating extracellular signal-regulated kinase. TUG-891-induced activation of human FFA4 also causes the receptor to internalize and phosphorylate quickly. [1]
In vitro, TUG-891 demonstrates potent agonist activity at FFA4. It stimulates Ca²⁺ mobilization in cells expressing the receptor. The compound also promotes the recruitment of β-arrestins and induces ERK phosphorylation, confirming its ability to activate multiple signaling pathways. It exhibits comparable signaling characteristics to the long-chain fatty acid α-linolenic acid. |
| ln Vivo |
TUG-891 rapidly lowers body weight and fat mass while increasing fat oxidation in C57Bl/6J mice by activating GPR120.[2]
In vivo, TUG-891 is used to explore the therapeutic potential of FFA4 agonism. Although specific in vivo efficacy data for TUG-891 are less detailed than for some other FFA4 agonists, its use in animal models helps to delineate the physiological roles of FFA4. By activating FFA4, the compound may influence insulin sensitivity, inflammation, and energy homeostasis. |
| Enzyme Assay |
In vitro enzyme or receptor binding (non-cell) assays for TUG-891 are used to determine its affinity and selectivity for FFA4. These assays involve incubating membrane preparations from cells expressing FFA4 with a radiolabeled ligand. The compound's ability to displace the radioligand is measured to calculate its Ki or IC50. Selectivity is confirmed by testing the compound against other receptors, such as FFA1.
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| Cell Assay |
The measured response is considered the peak signal over a 1.5-minute period following TUG-891 treatment, during which intracellular Ca2+ is monitored. Flp-In T-REx cell lines or HT-29 cells following a 5-minute TUG-891 treatment are used to measure the phosphorylation of extracellular signal-regulated kinase 1/2 (ERK). To observe the internalization of FFA4, human FFA4-eYFP Flp-In T-REx cells are grown on glass coverslips coated with poly-d-lysine. These cells are cultured for a full day prior to being treated with 100 ng/ml of doxycycline to enhance receptor expression. With confocal microscopy, live cells are imaged subsequent to TUG-891 addition.
In vitro cell-based assays for TUG-891 involve measuring its functional activity at FFA4. Cells expressing the receptor are treated with the compound, and various downstream signaling events are monitored. For example, intracellular calcium levels can be measured using fluorescent dyes, and β-arrestin recruitment can be assessed using enzyme complementation assays. ERK phosphorylation is detected by Western blotting. |
| Animal Protocol |
In vivo animal experiments for TUG-891 are conducted in rodent models to study the effects of FFA4 activation. The compound is typically administered orally or intraperitoneally. Outcome measures may include glucose tolerance tests, insulin sensitivity measurements, and assessment of inflammatory markers. The specific experimental design depends on the research question being addressed.
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| ADME/Pharmacokinetics |
Pharmacokinetic (PK) properties of TUG-891 have been characterized to support its use as a research tool. The compound has a molecular weight of 364.41 and a formula of C₂₃H₂₁FO₃. It is soluble in DMSO. As a small molecule, it is expected to have reasonable oral bioavailability, though specific parameters like half-life and clearance are determined in preclinical studies.
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| Toxicity/Toxicokinetics |
Toxicology (toxicology) data for TUG-891 are typical of a research compound. It is generally well-tolerated at effective doses. The safety profile is being evaluated in the context of its use as a research tool to study FFA4 biology.
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| References | |
| Additional Infomation |
Other information: TUG-891 is a valuable research compound for studying the biology of FFA4/GPR120. It is available from various chemical suppliers for preclinical research purposes. The compound is of interest for its potential therapeutic applications in metabolic and inflammatory diseases.
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| Molecular Formula |
C23H21FO3
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|---|---|
| Molecular Weight |
364.4164
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| Exact Mass |
364.147
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| Elemental Analysis |
C, 75.81; H, 5.81; F, 5.21; O, 13.17
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| CAS # |
1374516-07-0
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| Related CAS # |
1374516-07-0
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| PubChem CID |
57522038
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| Appearance |
White to off-white solid powder
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| LogP |
5.397
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
27
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| Complexity |
453
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1C(C2C=CC(C)=CC=2)=C(COC2C=CC(CCC(=O)O)=CC=2)C=C(F)C=1
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| InChi Key |
LPGBXHWIQNZEJB-UHFFFAOYSA-N
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| InChi Code |
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)
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| Chemical Name |
3-[4-[[5-fluoro-2-(4-methylphenyl)phenyl]methoxy]phenyl]propanoic acid
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| Synonyms |
TUG-891; TUG 891; TUG891
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: 73~100 mg/mL (200.3~274.4 mM)
Ethanol: ~6 mg/mL |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.86 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.86 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (6.86 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 5% DMSO + 95% Corn oil: 0.9mg/ml (2.47mM) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.7441 mL | 13.7204 mL | 27.4409 mL | |
| 5 mM | 0.5488 mL | 2.7441 mL | 5.4882 mL | |
| 10 mM | 0.2744 mL | 1.3720 mL | 2.7441 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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