1. GPCR/G Protein
  2. Free Fatty Acid Receptor
  3. GPR40 agonist 4

GPR40 agonist 4 is a potent free fatty acid receptor 1 (FFA1/ GPR40) agonist with a pEC50 of 7.54.

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GPR40 agonist 4 Chemical Structure

GPR40 agonist 4 Chemical Structure

CAS No. : 2102196-57-4

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10 mM * 1 mL in DMSO
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Customer Review

Based on 1 publication(s) in Google Scholar

Top Publications Citing Use of Products
  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

GPR40 agonist 4 is a potent free fatty acid receptor 1 (FFA1/ GPR40) agonist with a pEC50 of 7.54.

IC50 & Target

pEC50: 7.54 (FFA1/GPR40)[1]

In Vitro

GPR40 agonist 4 tends to have a low risk of activating caspase-3/7[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Single oral administration of GPR40 agonist 4 (compound 20) robustly reduces the plasma glucose excursion and enhances insulin secretion during an oral glucose tolerance test (OGTT) in a dose-dependent manner from 1 to 10 mg/kg when GPR40 agonist 4 is dosed 60 min prior to the oral glucose challenge. The area under the curve of blood glucose (AUC0-120min) and blood insulin (AUC0-120min) reveal that the minimum effective dose of GPR40 agonist 4 is 3 mg/kg. The hyperglycemia state is also markedly improved in GPR40 agonist 4 (20 mg/kg) treated group[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

416.87

Formula

C21H17ClO5S

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

ClC1=CC=CC=C1C2=CC(COC3=CC=C(S(CC(O)=O)(=O)=O)C=C3)=CC=C2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 160 mg/mL (383.81 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3988 mL 11.9941 mL 23.9883 mL
5 mM 0.4798 mL 2.3988 mL 4.7977 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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g

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(per animal)

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References
Cell Assay
[1]

Human hepatocyte HepG2 cells are cultured at 37°C, 5% CO2 in DMEM supplemented with 10% fetal bovine serum, 50 μg/mL streptomycin and 50 IU/mL penicillin. Cells are seeded in a 96-well plate (2×104 cells/well) and cultured with GPR40 agonist 4 (compound 20) in DMEM for 24 h. FGPR40 agonist 4 is measured in three independent experiments[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

8 weeks old normal male SD rats after 1 week adaptation are fasted overnight (12 h), weighted, bled via the tail vein, and randomized into 5 groups (n=6 for each group). Rats are administrated orally with a single doses of vehicle (0.5% methylcellulose aqueous solution) or GPR40 agonist 4 (compound 20) (1, 3 and 10 mg/kg suspended in vehicle) and subsequently dosed orally with glucose aqueous solution (3 g/kg) after 60 min. Blood samples are collected immediately before drug administration (~60 min), before glucose challenge (0 min), and at 15, 30, 60 and 120 min post-dose. The blood glucose is measured by blood glucose test strips[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.3988 mL 11.9941 mL 23.9883 mL 59.9707 mL
5 mM 0.4798 mL 2.3988 mL 4.7977 mL 11.9941 mL
10 mM 0.2399 mL 1.1994 mL 2.3988 mL 5.9971 mL
15 mM 0.1599 mL 0.7996 mL 1.5992 mL 3.9980 mL
20 mM 0.1199 mL 0.5997 mL 1.1994 mL 2.9985 mL
25 mM 0.0960 mL 0.4798 mL 0.9595 mL 2.3988 mL
30 mM 0.0800 mL 0.3998 mL 0.7996 mL 1.9990 mL
40 mM 0.0600 mL 0.2999 mL 0.5997 mL 1.4993 mL
50 mM 0.0480 mL 0.2399 mL 0.4798 mL 1.1994 mL
60 mM 0.0400 mL 0.1999 mL 0.3998 mL 0.9995 mL
80 mM 0.0300 mL 0.1499 mL 0.2999 mL 0.7496 mL
100 mM 0.0240 mL 0.1199 mL 0.2399 mL 0.5997 mL
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GPR40 agonist 4 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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GPR40 agonist 4
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HY-103083
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