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Purity: ≥98%
TUG-891 is a potent and selective agonist of the free fatty acid receptor 4 (FFA4/GPR120), which displays both potential opportunity and possible challenges to therapeutic agonism. TUG-891-induced activation of human FFA4 also caused the receptor to internalize and phosphorylate quickly. Although TUG-891 was also a strong agonist of mouse FFA4, its limited selectivity over mouse FFA1 made its in vivo application in this species more challenging.
| Targets |
FFA4/GPR120
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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]
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| ln Vivo |
TUG-891 rapidly lowers body weight and fat mass while increasing fat oxidation in C57Bl/6J mice by activating GPR120.[2]
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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.
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| References |
| Molecular Formula |
C23H21FO3
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|---|---|
| Molecular Weight |
364.4164
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| Exact Mass |
364.15
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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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| Appearance |
Solid powder
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| SMILES |
CC1=CC=C(C=C1)C2=C(C=C(C=C2)F)COC3=CC=C(C=C3)CCC(=O)O
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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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