1. GPCR/G Protein
  2. GPR40
    GPR84
  3. Setogepram

Setogepram (Synonyms: PBI-4050)

Cat. No.: HY-100775A
Handling Instructions

Setogepram (PBI-4050) acts as an orally active agonist for GPR40 and as an antagonist or inverse agonist for GPR84. Setogepram (PBI-4050) decreases renal, liver and pancreatic fibrosis. Setogepram (PBI-4050) exerts anti-fibrotic, anti-inflammatory and anti-proliferative actions.

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

Setogepram Chemical Structure

Setogepram Chemical Structure

CAS No. : 1002101-19-0

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Description

Setogepram (PBI-4050) acts as an orally active agonist for GPR40 and as an antagonist or inverse agonist for GPR84[1]. Setogepram (PBI-4050) decreases renal, liver and pancreatic fibrosis[1][2]. Setogepram (PBI-4050) exerts anti-fibrotic, anti-inflammatory and anti-proliferative actions[2].

IC50 & Target

GPR40, GPR84[1]

In Vitro

Setogepram (PBI-4050; 500 µM; 24 hours) inhibits TGF-β (10 ng/mL)-activated human hepatic stellate cells (HSCs) proliferation[2].
Setogepram (PBI-4050; 250 or 500 µM; 24hours) dose-dependently arrests HSCs at the G0/G1 phase without inducing apoptosis[2].

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

Setogepram (PBI-4050; 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].

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.
Molecular Weight

206.28

Formula

C₁₃H₁₈O₂

CAS No.

1002101-19-0

SMILES

O=C(CC1=CC=CC(CCCCC)=C1)O

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Setogepram
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HY-100775A
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