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

Setogepram sodium salt (Synonyms: PBI-4050 sodium salt)

Cat. No.: HY-100775 Purity: 99.65%
Handling Instructions

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

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

Setogepram sodium salt Chemical Structure

Setogepram sodium salt Chemical Structure

CAS No. : 1254472-97-3

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10 mM * 1 mL in DMSO USD 242 In-stock
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100 mg USD 1600 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Setogepram sodium salt:

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Description

Setogepram sodium salt (PBI-4050 sodium salt) acts as an orally active agonist for GPR40 and as an antagonist or inverse agonist for GPR84[1]. Setogepram sodium salt decreases renal, liver and pancreatic fibrosis[1][2]. Setogepram sodium salt 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.
Clinical Trial
Molecular Weight

228.26

Formula

C₁₃H₁₇NaO₂

CAS No.

1254472-97-3

SMILES

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

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: 

H2O : ≥ 100 mg/mL (438.10 mM)

DMSO : ≥ 64 mg/mL (280.38 mM)

*"≥" 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
10 mM 0.4381 mL 2.1905 mL 4.3810 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 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

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

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

*All of the co-solvents are provided by MCE.
References

Purity: 99.65%

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Product name:
Setogepram sodium salt
Cat. No.:
HY-100775
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