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Fezagepras sodium

Cat. No. M28051
Fezagepras sodium Structure
Synonym:

Setogepram sodium; PBI-4050 sodium

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Biological Activity

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

Chemical Information
Molecular Weight 228.26
Formula C13H17NaO2
CAS Number 1254472-97-3
Form Solid
Solubility (25°C) Water ≥ 100 mg/mL
DMSO ≥ 64 mg/mL
Storage 4°C, dry, sealed
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Lin-Hai Chen, et al. J Med Chem. Modulation of the G-Protein-Coupled Receptor 84 (GPR84) by Agonists and Antagonists

[2] Frédéric Labéguère, et al. J Med Chem. Discovery of 9-Cyclopropylethynyl-2-(( S)-1-[1,4]dioxan-2-ylmethoxy)-6,7-dihydropyrimido[6,1- a]isoquinolin-4-one (GLPG1205), a Unique GPR84 Negative Allosteric Modulator Undergoing Evaluation in a Phase II Clinical Trial

[3] Jean-François Thibodeau, et al. Clin Sci (Lond). PBI-4050 via GPR40 activation improves adenine-induced kidney injury in mice

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Keywords: Fezagepras sodium, Setogepram sodium; PBI-4050 sodium supplier, GPR/FFAR, inhibitors, activators


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