Understand the source comparison
Mazdutide In Vitro Research: Comparison
GLP-1R EC50 0.2 nM 0.3 nM N/A Mazdutide matches native GLP-1 potency despite dual activity GCGR EC50 0.8 nM No activity 0.5 nM Retains strong glucagon receptor engagement Hepatic CPT1A upregulation 2.3-fold at 5 nM No effect 3.1-fold at 2 nM Dual agonism produ
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- GLP-1R EC50
- 0.2 nM
- 0.3 nM
- N/A
- Mazdutide matches native GLP-1 potency despite dual activity
- GCGR EC50
- 0.8 nM
- No activity
- 0.5 nM
- Retains strong glucagon receptor engagement
- Hepatic CPT1A upregulation
- 2.3-fold at 5 nM
- No effect
- 3.1-fold at 2 nM
- Dual agonism produces liver-specific fat oxidation
- Adipocyte lipolysis (% increase vs control)
- 37% at 10 nM
- 12% at 10 nM
- 54% at 5 nM
- Balanced lipolysis without pure catabolic excess
- Insulin sensitivity (GLUT4 translocation)
- Enhanced
- Impaired
- GLP-1 component preserves glucose uptake despite glucagon signaling
- Recommended assay cell line
- CHO-K1 (dual transfected GLP-1R + GCGR)
- CHO-GLP-1R
- CHO-GCGR
- Dual-receptor systems required for full characterization