1. GPCR/G Protein
  2. GPR40
  3. GPR40 agonist 4

GPR40 agonist 4 

Cat. No.: HY-103083 Purity: 98.97%
Handling Instructions

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

For research use only. We do not sell to patients.

GPR40 agonist 4 Chemical Structure

GPR40 agonist 4 Chemical Structure

CAS No. : 2102196-57-4

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Based on 1 publication(s) in Google Scholar

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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].

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].

Molecular Weight

416.87

Formula

C₂₁H₁₇ClO₅S

CAS No.

2102196-57-4

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 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 160 mg/mL (383.81 mM; Need ultrasonic and warming)

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
10 mM 0.2399 mL 1.1994 mL 2.3988 mL
*Please refer to the solubility information to select the appropriate solvent.
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
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Keywords:

GPR40 agonist 4GPR40Free fatty acid receptor 1FFAR1FFA1G-protein-coupled receptor 40Inhibitorinhibitorinhibit

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GPR40 agonist 4
Cat. No.:
HY-103083
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