2. GPCR/G Protein
  3. Free Fatty Acid Receptor GPR84
  4. Fezagepras sodium

Fezagepras sodium  (Synonyms: Setogepram sodium; PBI-4050 sodium)

Cat. No.: HY-100775 Purity: 99.65%
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Fezagepras (Setogepram) sodium acts as an orally active agonist for GPR40 and as an antagonist or inverse agonist for GPR84. Fezagepras sodium decreases renal, liver and pancreatic fibrosis. Fezagepras sodium exerts anti-fibrotic, anti-inflammatory and anti-proliferative actions.

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

Fezagepras sodium Chemical Structure

Fezagepras sodium Chemical Structure

CAS No. : 1254472-97-3

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10 mM * 1 mL in DMSO
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10 mg USD 170 In-stock
25 mg USD 320 In-stock
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Based on 1 publication(s) in Google Scholar

Other Forms of Fezagepras sodium:

Fezagepras sodium Related Antibodies

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Description

Fezagepras (Setogepram) sodium acts as an orally active agonist for GPR40 and as an antagonist or inverse agonist for GPR84[1]. Fezagepras sodium decreases renal, liver and pancreatic fibrosis[1][2]. Fezagepras sodium exerts anti-fibrotic, anti-inflammatory and anti-proliferative actions[2].

IC50 & Target

GPR40, GPR84[1]
In Vitro

Fezagepras sodium (500 μM; 24 hours) inhibits TGF-β (10 ng/mL)-activated human hepatic stellate cells (HSCs) proliferation[2].
Fezagepras sodium (250 or 500 μM; 24 hours) dose-dependently arrests HSCs at the G0/G1 phase without inducing apoptosis[2].

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

Fezagepras sodium Related Antibodies

Cell Proliferation Assay[2]

Cell Line: HSCs
Concentration: 250 or 500 µM
Incubation Time: 24 hours
Result: Inhibited TGF-β-activated HSC proliferation. TGF-β (10 ng/mL) increased HSC proliferation by 10%.

Cell Cycle Analysis[2]

Cell Line: HSCs
Concentration: 250 µM, 500 µM
Incubation Time: 24 hours
Result: Inhibited cell cycle progression.
In Vivo

Fezagepras sodium (100 mg/kg/day; gavage from 8-20 weeks of age) markedly decreases hyperglycemia and markedly improvea glucose tolerance in type 2 diabetes eNOS-/-db/db mice[1].·

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

Animal Model: Type 2 diabetes eNOS-/-db/db mice[1]
Dosage: 100 mg/kg/day
Administration: Given via daily gavage from 8-20 weeks
Result: Compared with vehicle-treated mice, hyperglycemia was markedly decreased, and glucose tolerance was markedly improved.
Clinical Trial
Molecular Weight

228.26

Formula

C13H17NaO2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(O[Na])CC1=CC(CCCCC)=CC=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

H2O : ≥ 100 mg/mL (438.10 mM)

DMSO : ≥ 64 mg/mL (280.38 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 4.3810 mL 21.9048 mL 43.8097 mL
5 mM 0.8762 mL 4.3810 mL 8.7619 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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.08 mg/mL (9.11 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.08 mg/mL (9.11 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  PBS

    Solubility: 120 mg/mL (525.72 mM); Clear solution; Need ultrasonic

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

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Purity & Documentation

Purity: 99.65%

SDS (252 KB)

COA (242 KB) HNMR (182 KB) LCMS (118 KB)

Handling Instructions (2659 KB)
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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO / H2O 1 mM 4.3810 mL 21.9048 mL 43.8097 mL 109.5242 mL
5 mM 0.8762 mL 4.3810 mL 8.7619 mL 21.9048 mL
10 mM 0.4381 mL 2.1905 mL 4.3810 mL 10.9524 mL
15 mM 0.2921 mL 1.4603 mL 2.9206 mL 7.3016 mL
20 mM 0.2190 mL 1.0952 mL 2.1905 mL 5.4762 mL
25 mM 0.1752 mL 0.8762 mL 1.7524 mL 4.3810 mL
30 mM 0.1460 mL 0.7302 mL 1.4603 mL 3.6508 mL
40 mM 0.1095 mL 0.5476 mL 1.0952 mL 2.7381 mL
50 mM 0.0876 mL 0.4381 mL 0.8762 mL 2.1905 mL
60 mM 0.0730 mL 0.3651 mL 0.7302 mL 1.8254 mL
80 mM 0.0548 mL 0.2738 mL 0.5476 mL 1.3691 mL
100 mM 0.0438 mL 0.2190 mL 0.4381 mL 1.0952 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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Fezagepras sodium 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.

Keywords:

Fezagepras1254472-97-3SetogepramPBI-4050PBI4050PBI 4050Free Fatty Acid ReceptorGPR84FFARG protein coupled receptor 84Inhibitorinhibitorinhibit

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