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

Fezagepras  (Synonyms: Setogepram; PBI-4050)

Cat. No.: HY-100775A Purity: 99.38%
SDS COA Handling Instructions Technical Support

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

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

Fezagepras Chemical Structure

Fezagepras Chemical Structure

CAS No. : 1002101-19-0

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Based on 1 publication(s) in Google Scholar

Other Forms of Fezagepras:

Fezagepras Related Antibodies

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  • Biological Activity

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Description

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

IC50 & Target

GPR40, GPR84[1]
In Vitro

Fezagepras (500 μM; 24 hours) inhibits TGF-β (10 ng/mL)-activated human hepatic stellate cells (HSCs) proliferation[2].
Fezagepras (250 or 500 μM; 24hours) 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 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 (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

206.28

Formula

C13H18O2
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C(CC1=CC=CC(CCCCC)=C1)O
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 : 60 mg/mL (290.87 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 4.8478 mL 24.2389 mL 48.4778 mL
5 mM 0.9696 mL 4.8478 mL 9.6956 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • 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: ≥ 5 mg/mL (24.24 mM); Suspended solution

    This protocol yields a suspended solution of ≥ 5 mg/mL (saturation unknown). Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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: ≥ 5 mg/mL (24.24 mM); Clear solution

    This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.
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.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
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).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.38%

SDS (393 KB)

COA (242 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. 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 1 mM 4.8478 mL 24.2389 mL 48.4778 mL 121.1945 mL
5 mM 0.9696 mL 4.8478 mL 9.6956 mL 24.2389 mL
10 mM 0.4848 mL 2.4239 mL 4.8478 mL 12.1194 mL
15 mM 0.3232 mL 1.6159 mL 3.2319 mL 8.0796 mL
20 mM 0.2424 mL 1.2119 mL 2.4239 mL 6.0597 mL
25 mM 0.1939 mL 0.9696 mL 1.9391 mL 4.8478 mL
30 mM 0.1616 mL 0.8080 mL 1.6159 mL 4.0398 mL
40 mM 0.1212 mL 0.6060 mL 1.2119 mL 3.0299 mL
50 mM 0.0970 mL 0.4848 mL 0.9696 mL 2.4239 mL
60 mM 0.0808 mL 0.4040 mL 0.8080 mL 2.0199 mL
80 mM 0.0606 mL 0.3030 mL 0.6060 mL 1.5149 mL
100 mM 0.0485 mL 0.2424 mL 0.4848 mL 1.2119 mL
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Fezagepras 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:

Fezagepras1002101-19-0Setogepram PBI-4050PBI4050PBI 4050PBI-4050Free Fatty Acid ReceptorGPR84FFARG protein coupled receptor 84Diabetes,Kidney,Renal,Pancreatic,Liver,Fibrosis,NephrologyInhibitorinhibitorinhibit

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