| Size | Price | |
|---|---|---|
| 100mg | ||
| 250mg | ||
| Other Sizes |
| Targets |
FFA3-Agonist-1 targets the free fatty acid receptor 3 (FFA3; also known as GPR41), a G protein-coupled receptor that is activated by short-chain fatty acids (SCFAs) produced by the intestinal microbiota. As a PAM-agonist, FFA3-Agonist-1 enhances the receptor's response to endogenous ligands and directly activates the receptor. Activation of FFA3 modulates various physiological processes, including energy homeostasis, inflammation, and hormone secretion.
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|---|---|
| ln Vitro |
Insertable [35S]GTPgS and pERK1/FFA3 agonist 1 (0.1-100 µM) increases the production of human free graft 3, mouse free graft 3 (mFFA3), rabbit graft 3 (rFFA3) 2, and decreases the production of cAMP. FFA3 agonist 1 (0.01-100 µM) increases the induction of expression of enhanced yellow fluorescent protein (eYFP) human free ion sorbent 3 (hFFA3) in Flp-in-T-REx 293 cells. [35S] GTPgS Self-importation [2].
FFA3-Agonist-1 (0.01-100 µM) increases the induction of expression of enhanced yellow fluorescent protein (eYFP) in Flp-in-T-REx 293 cells expressing human FFA3 (hFFA3). Its activity can be assessed using cell-based assays in which cells expressing the human FFA3 receptor are treated with the compound and receptor activation is measured by quantifying reporter gene expression or downstream signaling. |
| ln Vivo |
FFA3-Agonist-1 is used as a research tool to study the role of FFA3 in mediating the health-promoting effects of the intestinal microbiota. By activating FFA3, the compound can be used to investigate the effects of FFA3 signaling on metabolism, inflammation, and other physiological processes. The compound's in vivo activity has been characterized in animal models.
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| Enzyme Assay |
Non-cellular receptor binding assays for FFA3-Agonist-1 involve competitive radioligand binding displacement studies using membrane preparations from cells expressing the human FFA3 receptor. The membranes are incubated with a radiolabeled FFA3 ligand and varying concentrations of FFA3-Agonist-1. Following incubation and filtration, the radioactivity is measured to determine the IC50, which is then converted to a Ki value using the Cheng-Prusoff equation.
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| Cell Assay |
In vitro cellular assays for FFA3-Agonist-1 involve treating cells expressing the human FFA3 receptor (e.g., Flp-in-T-REx 293 cells) with the compound and measuring receptor-mediated signaling. Cells are treated with varying concentrations of FFA3-Agonist-1 (0.01-100 µM), and the activation of the receptor is measured by quantifying the expression of a reporter gene (e.g., eYFP) or by measuring downstream signaling such as calcium mobilization or cAMP modulation. The EC50 for receptor activation is determined from dose-response curves.
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| Animal Protocol |
In vivo animal experiments with FFA3-Agonist-1 are conducted in rodent models to study the role of FFA3 in mediating the effects of the intestinal microbiota. Animals are treated with FFA3-Agonist-1 via oral or intraperitoneal administration, and parameters such as metabolic rate, insulin sensitivity, inflammation markers, and gut hormone levels are measured. The compound's effects on microbiota composition and function may also be assessed.
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| ADME/Pharmacokinetics |
FFA3-Agonist-1 has a molecular weight of 362.42 and a molecular formula of C22H22N2O3. It is a solid at room temperature and is typically stored at -20°C. Purity is typically 95%. The compound is soluble in DMSO and other organic solvents. It is stable under recommended storage conditions.
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| Toxicity/Toxicokinetics |
FFA3-Agonist-1 is a research compound for laboratory use only and is not intended for human therapeutic or diagnostic use. Standard laboratory safety precautions should be followed when handling the compound. It may cause skin, eye, and respiratory irritation. Appropriate personal protective equipment should be used.
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| References |
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| Additional Infomation |
FFA3-Agonist-1 (CAS 886358-51-6) is a free fatty acid receptor 3 (FFA3) agonist and a selective, moderately potent positive allosteric modulator (PAM)-agonist of the FFA3 receptor. It modulates the health effects of the intestinal microbiota through activation of FFA3. The compound is available from various commercial suppliers for research applications.
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| Molecular Formula |
C22H22N2O3
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|---|---|
| Molecular Weight |
362.421685695648
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| Exact Mass |
362.163
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| CAS # |
886358-51-6
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| PubChem CID |
11646235
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| Appearance |
Off-white to light yellow solid powder
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| LogP |
2.9
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
27
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| Complexity |
694
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C(C1C(C2=CC=CO2)C2C(CCCC=2NC=1C)=O)NC1C(C)=CC=CC=1
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| InChi Key |
HIWQJAGWEWRIIP-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C22H22N2O3/c1-13-7-3-4-8-15(13)24-22(26)19-14(2)23-16-9-5-10-17(25)20(16)21(19)18-11-6-12-27-18/h3-4,6-8,11-12,21,23H,5,9-10H2,1-2H3,(H,24,26)
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| Chemical Name |
4-(furan-2-yl)-2-methyl-N-(2-methylphenyl)-5-oxo-4,6,7,8-tetrahydro-1H-quinoline-3-carboxamide
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| Synonyms |
FFA3-Agonist 1; FFA3-Agonist1; FFA3-Agonist-1
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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 : ~25 mg/mL (~68.98 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.90 mM) (saturation unknown) in 10% DMSO + 40% PEG300 +5% Tween-80 + 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.7592 mL | 13.7961 mL | 27.5923 mL | |
| 5 mM | 0.5518 mL | 2.7592 mL | 5.5185 mL | |
| 10 mM | 0.2759 mL | 1.3796 mL | 2.7592 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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