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pegozafermin   Click here for help

GtoPdb Ligand ID: 14215

Compound class: Peptide
Comment: Pegozafermin (BIO89-100; originally from 89bio, now Roche) is a human FGF-21 analogue. It is O-glycosylated and PEGylated to extend circulating half-life, and has amino acid substitution R175>A to increase receptor potency [1,3]. It was designed to mimic the effects of FGF-21/FGFR signalling for clinical benefit in metabolic disorders (insulin resistance, hypertriglyceridemia, fatty liver disease, inflammation-driven fibrotic liver scarring, and obesity) [3].
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Bioactivity Comments
Pegozafermin activates fibroblast growth factor receptors (FGFRs) 1-3, but not FGFR4 in vitro [3].
Selectivity at catalytic receptors
Key to terms and symbols Click column headers to sort
Target Sp. Type Action Value Parameter Concentration range (M) Reference
fibroblast growth factor receptor 1 Hs Agonist Agonist 9.2 pEC50 - 3
pEC50 9.2 (EC50 6x10-10 M) [3]
Description: Determined in rat L6 cells expressing human FGFR1c/β-Klotho, measuring downstream ERK phosphorylation