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Fezagepras

Cat. No. M27599
Fezagepras Structure
Synonym:

Setogepram; PBI-4050

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Biological Activity

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

Chemical Information
Molecular Weight 206.28
Formula C13H18O2
CAS Number 1002101-19-0
Storage Please store the product under the recommended conditions in the Certificate of Analysis.
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] Jean-François Thibodeau, et al. Clin Sci (Lond). PBI-4050 via GPR40 activation improves adenine-induced kidney injury in mice

[3] Quang T Nguyen, et al. Cardiovasc Res. PBI-4050 reduces pulmonary hypertension, lung fibrosis, and right ventricular dysfunction in heart failure

[4] Nasreen Khalil, et al. Eur Respir J. Phase 2 clinical trial of PBI-4050 in patients with idiopathic pulmonary fibrosis

[5] Yan Li, et al. JCI Insight. Fatty acid receptor modulator PBI-4050 inhibits kidney fibrosis and improves glycemic control

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


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