For research use only. Not for therapeutic Use.
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].
PF-739 activates α2β1γ1, α2β2γ1, α1β1γ1 and α1β2γ1 with EC50 values of 5.23 nM, 42.2 nM, 8.99 nM and 126 nM, respectively[1].
PF-739 (0-1000 nM) increases the phosphorylation of AMPK substrate in primary rat hepatocytes and myotubes of primary human cardiac cell line with dose-dependent manner[2].
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].
| Catalog Number | I034534 |
| CAS Number | 1852452-14-2 |
| Synonyms | (3R,3aR,6R,6aR)-6-[[6-chloro-5-[4-[1-(hydroxymethyl)cyclopropyl]phenyl]-1H-benzimidazol-2-yl]oxy]-2,3,3a,5,6,6a-hexahydrofuro[3,2-b]furan-3-ol |
| Molecular Formula | C23H23ClN2O5 |
| Purity | ≥95% |
| InChI | InChI=1S/C23H23ClN2O5/c24-15-8-17-16(7-14(15)12-1-3-13(4-2-12)23(11-27)5-6-23)25-22(26-17)31-19-10-30-20-18(28)9-29-21(19)20/h1-4,7-8,18-21,27-28H,5-6,9-11H2,(H,25,26)/t18-,19-,20-,21-/m1/s1 |
| InChIKey | IMVYDTHPRTUISR-XRXFAXGQSA-N |
| SMILES | C1CC1(CO)C2=CC=C(C=C2)C3=CC4=C(C=C3Cl)NC(=N4)OC5COC6C5OCC6O |
| Reference | [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. |
