| Chemical Properties | Back Directory | [Boiling point ]
694.0±65.0 °C(Predicted) | [density ]
1.479±0.06 g/cm3(Predicted) | [form ]
Solid | [pka]
8.93±0.10(Predicted) | [color ]
Off-white to light yellow |
| Hazard Information | Back Directory | [Description]
PF-739 is an AMPK agonist. It has been shown to activate AMPK in hepatocytes and skeletal muscle. | [Uses]
PF-739 is an orally active and non-selective activator of AMPK. PF-739 activates 12 heterotrimeric AMPK complexes and significantly reduces the level of glucose in plasma complexes[1][2]. | [in vivo]
PF-739 (30-1000 mg/kg; p.o. or s.c.; single does) effectively activates AMPK in liver cells and skeletal muscle and reduces plasma glucose level in C57BL/6 mice[2]. | Animal Model: | C57BL/6 mice[2]. | | Dosage: | 30, 100, 300 or 1000 mg/kg. | | Administration: | Oral gavage or subcutaneous injection; single does. | | Result: | Increased AMPK activity in skeletal muscle, AMPK phosphorylation in liver tissue and the expression of transcription factors Ppargc1a, Nr4a1, Nr4a3 in glucose metabolism pathway, and decreased plasma insulin and blood glucose. |
| [IC 50]
AMPK α1β1γ1: 8.99 nM (EC50); AMPK α1β2γ1: 126 nM (EC50); AMPK α2β1γ1: 5.23 nM (EC50); AMPK α2β2γ1: 42.2 nM (EC50) | [References]
[1] Aledavood E, et al. Elucidating the Activation Mechanism of AMPK by Direct Pan-Activator PF-739[J]. Frontiers in Molecular Biosciences, 2021, 8: 760026.
[2] Cokorinos EC, et al. Activation of Skeletal Muscle AMPK Promotes Glucose Disposal and Glucose Lowering in Non-human Primates and Mice. Cell Metab. 2017 May 2;25(5):1147-1159.e10. DOI:10.1016/j.cmet.2017.04.010 |
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