| 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 |
| Targets |
logEC50: −7.62[1]
GPR120 Compound A specifically targets the G protein-coupled receptor 120 (GPR120), a lipid-sensing receptor. It acts as a potent and selective agonist, activating GPR120 with an EC50 of approximately 0.35 µM. This activation is believed to have beneficial effects on hepatic lipid metabolism, leading to decreased liver triglycerides and hepatic steatosis. Its selectivity over GPR40 is a key feature of its mechanism. |
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| ln Vitro |
GPR120 Agonist 3 has minimal activity towards Gpr40 and complete selectivity for Gpr120 (logEC50=−7.62). Both human and mouse Gpr120 expressing cells generate concentration-dependent increases in IP3 synthesis when exposed to GPR120 Agonist 3. With EC50s of approximately 0.35 μM, GPR120 Agonist 3 causes β-arrestin-2 to be recruited in both human and mouse Gpr120 expressing cells in a concentration-dependent manner. GPR120 Agonist 3 suppresses LPS-induced phosphorylation of Tak1, Ikkβ, and Jnk and prevents IκB degradation in a strong and comparable manner [1].
In vitro, GPR120 Compound A is a potent agonist of GPR120. It activates GPR120 with a logEC50 of -7.62 and an EC50 of approximately 0.35 µM. Its activity is characterized by its ability to selectively activate GPR120 over GPR40. This makes it a valuable tool for studying the specific signaling pathways activated by GPR120. |
| ln Vivo |
Only in WT mice, GPR120 Agonist 3 improves insulin sensitivity by raising glucose infusion rates, insulin-stimulated glucose disposal rates, and insulin's capacity to suppress hepatic glucose synthesis. Treatment with GPR120 Agonist 3 improves hepatic lipid metabolism by reducing liver triglycerides, DAGs, and hepatic steatosis, as well as the content of saturated free fatty acids[1].
In vivo, GPR120 Compound A has been shown to have beneficial effects on hepatic lipid metabolism. It causes decreased liver triglycerides, decreased hepatic steatosis, and decreased saturated free fatty acid content. These findings suggest that GPR120 agonism could be a therapeutic strategy for treating metabolic dysfunction-associated steatotic liver disease (MASLD) and related conditions. |
| Enzyme Assay |
In vitro enzyme/receptor binding studies for GPR120 Compound A are not typical, as it is a receptor agonist. Its activity is assessed in cell-based functional assays. In these assays, cells expressing GPR120 are treated with the compound, and receptor activation is measured by downstream signaling events, such as calcium mobilization or cAMP modulation. The EC50 of approximately 0.35 µM is determined from these experiments.
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| Cell Assay |
In vitro cellular assays for GPR120 Compound A are the primary method for evaluating its activity. In these experiments, cells expressing GPR120 are treated with the compound, and the activation of the receptor is measured. Key readouts include the mobilization of intracellular calcium, which is a common signaling pathway for G protein-coupled receptors. These assays confirm the compound's mechanism as a potent GPR120 agonist.
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| Animal Protocol |
Mice: Male C57Bl/6 WT or Gpr120 KO littermates are fed a normal
chow (13.5% fat) or high-fat diet (60% fat) ad libitum for 15-20 weeks
from 8 weeks of age. After 15 weeks on HFD, WT and Gpr120 KO mice are
switched to an isocaloric HFD supplemented with ω3-FA concentrate or 30
mg/kg GPR120-IN-1 and fed for 5 weeks. Mice receive fresh diet every 3rd
day, and food consumption and body weight are monitored[1].
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of GPR120 Compound A are characterized by its oral availability. It has a molecular weight of 405.84 g/mol and a molecular formula of C₁₉H₂₃ClF₃NO₃. It is soluble in DMSO and ethanol. These properties are favorable for an orally administered compound and are important for its use in in vivo studies.
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| Toxicity/Toxicokinetics |
Toxicological data for GPR120 Compound A are limited, as it is a research compound. Its primary value is as a tool for studying GPR120 biology. While specific toxicity profiles are not detailed, its mechanism of activating a lipid-sensing receptor could have metabolic effects. Comprehensive safety studies are not available in the public domain.
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| References | |
| Additional Infomation |
GPR120 Compound A is a research-use-only compound that acts as a potent and selective GPR120 agonist. Its CAS number is 1599477-75-4. It is also known as GPR120-IN-1 and has the chemical name 2-{3-[2-chloro-5-(trifluoromethoxy)phenyl]-3-azaspiro[5.5]undecan-9-yl}acetic acid. This compound is a valuable tool for researchers studying the role of GPR120 in metabolism and related diseases. It is not an approved drug.
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| Molecular Formula |
C19H23CLF3NO3
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|---|---|
| Molecular Weight |
405.839035272598
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| Exact Mass |
405.132
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| CAS # |
1599477-75-4
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| PubChem CID |
73777063
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| Appearance |
White to off-white solid powder
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| LogP |
5.555
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
27
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| Complexity |
513
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
WUJVPELCYCESAP-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C19H23ClF3NO3/c20-15-2-1-14(27-19(21,22)23)12-16(15)24-9-7-18(8-10-24)5-3-13(4-6-18)11-17(25)26/h1-2,12-13H,3-11H2,(H,25,26)
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| Chemical Name |
2-[3-[2-chloro-5-(trifluoromethoxy)phenyl]-3-azaspiro[5.5]undecan-9-yl]acetic acid
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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 : ≥ 50 mg/mL (~123.20 mM)
H2O : < 0.1 mg/mL |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.16 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 (6.16 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 (6.16 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4640 mL | 12.3201 mL | 24.6403 mL | |
| 5 mM | 0.4928 mL | 2.4640 mL | 4.9281 mL | |
| 10 mM | 0.2464 mL | 1.2320 mL | 2.4640 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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