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GPR120 Agonist 2

Alias: GPR120 Agonist 2; MDK4111; MDK-4111; MDK 4111
Cat No.:V3100 Purity: ≥98%
GPR120 Agonist 2 is a potent and selective agonist of the GPR120 (G-protein coupled receptor) receptor.
GPR120 Agonist 2
GPR120 Agonist 2 Chemical Structure CAS No.: 1234844-11-1
Product category: Free Fatty Acid Receptor
This product is for research use only, not for human use. We do not sell to patients.
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

GPR120 Agonist 2 is a potent and selective agonist of the GPR120 (G-protein coupled receptor) receptor. It is taken from example 209 of patent US 20110313003 A1. The human GPR120 gene encodes GPR 120, a protein belonging to the rhodopsin family. GPR120 has also been shown to mediate the anti-inflammatory and insulin-sensitizing effects of omega 3 fatty acids. Obesity results from decreased fat metabolism, which is caused by a lack of GPR120.

Biological Activity I Assay Protocols (From Reference)
Targets
GPR120
GPR120 Agonist 2 is not mentioned in the literature, and the GPR120 receptor agonists involved in the literature target the GPR120 receptor [1]
ln Vitro

In vitro activity: GPR120 Agonist 2, a GPR120 agonist, is helpful in treating metabolic disorders, such as Type II diabetes and conditions linked to inadequate glycemic control[1].


The GPR120 receptor agonists can also promote the secretion of glucagon - like peptide - 1 (GLP - 1) in intestinal endocrine cells in vitro[1]
ln Vivo

The agonists can also improve insulin sensitivity in obese animal models, reducing insulin resistance caused by metabolic disorders[1]
Enzyme Assay
Treatment for metabolic disorders, such as Type II diabetes and conditions linked to inadequate glycemic control, can be achieved with GPR120 Agonist 2.
After the cells adhere to the plate, different concentrations of the agonists are added and incubated for a specified period. Then, a calcium ion - sensitive fluorescent probe is added to the system. The fluorescence intensity changes caused by calcium ion mobilization activated by the combination of the agonists and the GPR120 receptor are detected by a fluorescence detector to evaluate the agonist activity of the compounds[1]
Cell Assay
The cultured cells are divided into experimental groups and control groups. The experimental groups are treated with different doses of GPR120 receptor agonists, while the control groups are treated with equal volumes of solvent without the agonists. After continuous incubation for a certain time, the cell culture supernatant is collected
The content of GLP - 1 in the supernatant is detected by a specific immunoassay method to determine the ability of the agonists to promote GLP - 1 secretion from intestinal endocrine cells[1]
Animal Protocol

The drug - treated groups are given different oral doses of GPR120 receptor agonists once a day, and the control group is given the same volume of solvent. During the experimental period, the mice are fed a high - fat diet to maintain the metabolic disorder model. The body weight, fasting blood glucose and insulin levels of the mice are measured regularly within a set experimental cycle[1]
References

[1]. Gpr120 receptor agonists and uses thereof. US20110313003.

Additional Infomation
Its mechanism of action is mainly through activating GPR120 receptors to regulate the secretion of intestinal hormones (such as GLP-1), improve insulin sensitivity, and regulate glucose and lipid metabolism, thereby achieving the effect of treating metabolic disorders [1]
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C22H25CLO4
Molecular Weight
388.89
Exact Mass
388.14
Elemental Analysis
C, 67.95; H, 6.48; Cl, 9.12; O, 16.46
CAS #
1234844-11-1
Related CAS #
1234844-11-1
PubChem CID
46700745
Appearance
White to off-white solid powder
LogP
5.1
Hydrogen Bond Donor Count
1
Hydrogen Bond Acceptor Count
4
Rotatable Bond Count
6
Heavy Atom Count
27
Complexity
522
Defined Atom Stereocenter Count
0
InChi Key
KOHMUAMPZUHGNV-UHFFFAOYSA-N
InChi Code
InChI=1S/C22H25ClO4/c1-13-14(2)19(7-5-15(13)6-8-20(24)25)26-12-17-10-18(23)9-16-11-22(3,4)27-21(16)17/h5,7,9-10H,6,8,11-12H2,1-4H3,(H,24,25)
Chemical Name
3-[4-[(5-chloro-2,2-dimethyl-3H-1-benzofuran-7-yl)methoxy]-2,3-dimethylphenyl]propanoic acid
Synonyms
GPR120 Agonist 2; MDK4111; MDK-4111; MDK 4111
HS Tariff Code
2934.99.9001
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)
Solubility Data
Solubility (In Vitro)
DMSO: ≥ 50 mg/mL (~128.6 mM)
Water: <1mg/mL
Ethanol: <1mg/mL
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 3.5 mg/mL (9.00 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 35.0 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: ≥ 3.5 mg/mL (9.00 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 35.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.5714 mL 12.8571 mL 25.7142 mL
5 mM 0.5143 mL 2.5714 mL 5.1428 mL
10 mM 0.2571 mL 1.2857 mL 2.5714 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.

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What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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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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