| Size | Price | Stock | Qty |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 500mg | |||
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| Other Sizes |
| Targets |
Setogepram targets GPR40 (as an agonist) and GPR84 (as an antagonist or inverse agonist).
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| ln Vitro |
Human hepatic stellate cell (HSC) proliferation stimulated by TGF-β (10 ng/mL) is inhibited by fezagepras (500 µM; 24 hours) [2]. HSCs in the G0/G1 phase are dose-dependently arrested by fezagepras (250 or 500 µM; 24 hours) without causing apoptosis [2].
In vitro, Setogepram demonstrates activity at its targets, GPR40 and GPR84. It has been shown to reduce fibrosis in cellular models. Its anti-proliferative effects have been observed in various cell-based assays. |
| ln Vivo |
In type 2 diabetic eNOS-/-db/db mice, fezagepras (100 mg/kg/day; gavage commencing from 8–20 weeks of age) can considerably increase glucose tolerance and reduce hyperglycemia [1].
In vivo, Setogepram has been shown to reduce renal, hepatic, and pancreatic fibrosis in animal models. It exerts anti-fibrotic, anti-inflammatory, and anti-proliferative actions in vivo. |
| Enzyme Assay |
In vitro receptor binding and functional assays for Setogepram involve measuring its activity at GPR40 and GPR84. For GPR40 agonism, cells expressing the receptor are treated with the compound, and downstream signaling (e.g., calcium flux or cAMP modulation) is measured. For GPR84 antagonism, the compound's ability to inhibit agonist-induced responses is assessed. These assays typically use radio-labeled ligands or fluorescent probes.
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| Cell Assay |
Cell Proliferation Assay[2]
Cell Types: HSC Tested Concentrations: 250 or 500 µM Incubation Duration: 24 hrs (hours) Experimental Results: Inhibition of TGF-β activated HSC 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. In vitro cellular assays for Setogepram are conducted using fibrotic cell models, such as hepatic stellate cells or renal fibroblasts stimulated with pro-fibrotic factors (e.g., TGF-β). Cells are treated with the compound, and markers of fibrosis (e.g., collagen, α-SMA) are quantified by qPCR or Western blot. Anti-inflammatory activity is assessed in macrophages by measuring cytokine production (e.g., TNF-α, IL-6) upon LPS stimulation. |
| Animal Protocol |
Animal/Disease Models: Type 2 diabetic eNOS-/-db/db mice[1]
Doses: 100 mg/kg/day Route of Administration: Daily gavage from 8-20 weeks Experimental Results: Compared with vehicle-treated mice, Hyperglycemia was Dramatically diminished, and glucose tolerance was Dramatically improved. In vivo animal studies for Setogepram employ models of organ fibrosis, such as unilateral ureteral obstruction (UUO) for renal fibrosis, carbon tetrachloride (CCl4)-induced liver fibrosis, or streptozotocin-induced diabetes for pancreatic fibrosis. The compound is administered orally, and endpoints include histological analysis of fibrosis, biochemical markers (e.g., collagen content), and inflammatory cell infiltration. |
| ADME/Pharmacokinetics |
Setogepram is orally bioactive, indicating good oral bioavailability. Its PK properties have been characterized in preclinical species, showing systemic exposure following oral administration. It is designed for oral delivery, with a favorable profile for chronic administration in fibrotic diseases.
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| Toxicity/Toxicokinetics |
Toxicological data for Setogepram are not detailed in publicly available sources; however, as it has been in clinical development, it would have undergone standard preclinical safety pharmacology and toxicology assessments. These would include acute and repeat-dose toxicity studies in at least two species, as well as genotoxicity and safety pharmacology profiling.
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| References |
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| Additional Infomation |
Setogepram is being studied in the clinical trial NCT03184584 (PBI 4050, an open-label rolling study in patients with Alström syndrome).
Setogepram is also known as Fezagepras and PBI-4050. It is a first-in-class dual modulator of GPR40 and GPR84 being developed for the treatment of fibrotic diseases. It has been investigated in clinical trials for conditions like idiopathic pulmonary fibrosis (IPF) and other fibrotic disorders. It has not yet received regulatory approval for marketing. |
| Molecular Formula |
C13H18O2
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|---|---|
| Molecular Weight |
206.280824184418
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| Exact Mass |
206.131
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| CAS # |
1002101-19-0
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| Related CAS # |
Fezagepras sodium;1254472-97-3
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| PubChem CID |
24749700
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| Appearance |
Off-white to light yellow solid powder
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| LogP |
3.046
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
15
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| Complexity |
189
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| Defined Atom Stereocenter Count |
0
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| SMILES |
OC(CC1=CC=CC(=C1)CCCCC)=O
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| InChi Key |
PEGQOIGYZLJMIB-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C13H18O2/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)
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| Chemical Name |
2-(3-pentylphenyl)acetic acid
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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 |
| 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 | |
| 10 mM | 0.4848 mL | 2.4239 mL | 4.8478 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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