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GPR120 Compound A is a novel, oral and potent agonist of GPR120 (logEC50 = −7.62). GPR120 compound A activated GPR120 with the EC50 value of ~0.35 μM. GPR120 compound A demonstrated potent selectivity over another lipid-sensing G-protein, GPR40 (FFAR1). In a high-fat diet fed obese mice, GPR120 compound A (30 mg/kg) exerted anti-inflammatory effects on macrophages in vitro and improved glucose tolerance, decreased hyperinsulinemia, increased insulin sensitivity, and decreased hepatic steatosis.
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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].
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| 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].
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| References |
| 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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