| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| 250mg | |||
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| Targets |
Setogepram sodium targets the G protein-coupled receptors GPR40 and GPR84. GPR40 (free fatty acid receptor 1) is primarily expressed in pancreatic β-cells and enteroendocrine cells, where it mediates fatty acid-induced insulin secretion. GPR84 is a medium-chain fatty acid receptor involved in inflammation and fibrosis. As a GPR40 agonist, setogepram enhances insulin secretion. As a GPR84 antagonist/inverse agonist, it reduces fibrosis and inflammation.
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| ln Vitro |
Fizagoprazole (500 μM; 24 hours) suppresses the proliferation of human hepatic stellate cells (HSCs) stimulated by TGF-β (10 ng/mL) [2].
In vitro, setogepram sodium (500 μM; 24 hours) suppresses the proliferation of human hepatic stellate cells (HSCs) stimulated by TGF-β (10 ng/mL). It inhibits the activation and proliferation of HSCs, which are key cells in liver fibrosis. It also blocks HSCs in the G0/G1 phase without inducing cell death. These activities demonstrate its anti-fibrotic potential. |
| ln Vivo |
In individuals with type 2 diabetes, fizagopra sodium (100 mg/kg/day; gavage commencing at 8–20 weeks of age) dramatically improves eNOS-/-db/db drought tolerance and considerably lowers hyperglycemia [1]. eNOS-/-db/db mice with type 2 diabetes [1]
In vivo, setogepram sodium (100 mg/kg/day; gavage for 12 weeks) significantly improves glucose tolerance and markedly lowers hyperglycemia in eNOS⁻/⁻db/db mice, a model of type 2 diabetes. It reduces renal, liver, and pancreatic fibrosis. These findings support its therapeutic potential for fibrotic diseases and diabetes. |
| Enzyme Assay |
In vitro receptor binding/functional assays for setogepram sodium are performed using cells expressing human GPR40 or GPR84. For GPR40 agonism, cells are loaded with a calcium-sensitive dye, and calcium mobilization is measured upon compound addition. For GPR84 antagonism/inverse agonism, cells are stimulated with a GPR84 agonist, and inhibition of signaling is measured. EC50 and IC50 values are calculated from dose-response curves.
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| Cell Assay |
Cell Proliferation Assay[2]
Cell Types: HSCs Tested Concentrations: 250 or 500 µM Incubation Duration: 24 hrs (hours) Experimental Results: Inhibits TGF-β-activated HSCs. Blocks HSCs in the G0/G1 phase without inducing cell trade[2]. proliferation. TGF-β (10 ng/mL) increased HSC proliferation by 10%. Cell Cycle Assay[2] Cell Types: HSC Tested Concentrations: 250 µM, 500 µM Incubation Duration: 24 hrs (hours) Experimental Results: Inhibition of cell cycle progression. For in vitro cellular assays, human hepatic stellate cells (HSCs) are stimulated with TGF-β (10 ng/mL) to induce proliferation. The cells are treated with setogepram sodium (250 or 500 µM) for 24 hours. Cell proliferation is assessed by cell counting or MTT assays. Cell cycle analysis is performed by flow cytometry. These assays confirm the compound's anti-fibrotic and anti-proliferative activity. |
| Animal Protocol |
Animal/Disease Models: Type 2 diabetes eNOS-/-db/db mice[1]
Doses: 100 mg/kg/day Route of Administration: Given via daily gavage from 8-20 weeks Experimental Results:Compared with vehicle-treated mice, hyperglycemia was markedly diminished, and glucose tolerance was markedly improved. In vivo animal studies for setogepram sodium are conducted in eNOS⁻/⁻db/db mice, a model of type 2 diabetes. The compound is administered via oral gavage at 100 mg/kg/day from 8 to 20 weeks of age. Blood glucose levels, glucose tolerance, and markers of fibrosis in the kidney, liver, and pancreas are assessed. Efficacy is compared to vehicle-treated mice. |
| ADME/Pharmacokinetics |
Setogepram sodium has a molecular weight of 228.26 g/mol and a molecular formula of C13H17NaO2. It is a white to off-white solid powder. It is typically stored as a powder at -20°C for up to 3 years or in solvent at -80°C for up to 6 months. It is orally bioactive. Detailed pharmacokinetic parameters, such as half-life and bioavailability, would be determined in preclinical studies.
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| Toxicity/Toxicokinetics |
Preclinical toxicity of setogepram sodium would be evaluated in standard toxicology studies. As a GPR40 agonist and GPR84 antagonist, potential adverse effects may include gastrointestinal effects and effects on lipid metabolism. In animal studies, it has shown a favorable safety profile at therapeutic doses. Comprehensive toxicity data is not widely available in public databases.
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| References |
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| Additional Infomation |
Setogepram sodium (Fezagepras, PBI-4050) is an orally bioactive GPR40 agonist and GPR84 antagonist/inverse agonist. It reduces fibrosis in the kidney, liver, and pancreas. It has anti-inflammatory and anti-proliferative effects. It is available for research purposes only.
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| Molecular Formula |
C13H17NAO2
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| Molecular Weight |
228.26265501976
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| Exact Mass |
228.112
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| CAS # |
1254472-97-3
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| Related CAS # |
Fezagepras;1002101-19-0
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| PubChem CID |
46944243
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
16
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| Complexity |
194
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
CNSJWSLXKSJQFE-UHFFFAOYSA-M
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| InChi Code |
InChI=1S/C13H18O2.Na/c1-2-3-4-6-11-7-5-8-12(9-11)10-13(14)15;/h5,7-9H,2-4,6,10H2,1H3,(H,14,15);/q;+1/p-1
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| Chemical Name |
sodium;2-(3-pentylphenyl)acetate
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
H2O : ≥ 100 mg/mL (~438.10 mM)
DMSO : ≥ 64 mg/mL (~280.38 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (9.11 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 20.8 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: ≥ 2.08 mg/mL (9.11 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (9.11 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 120 mg/mL (525.72 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 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 | |
| 10 mM | 0.4381 mL | 2.1905 mL | 4.3810 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.
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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