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MedChemExpressModel PF-739 -1852452-14-2

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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].
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PF-739

MCE China:PF-739

Brand:MedChemExpress (MCE)

Cat. No.HY-117755

CAS:1852452-14-2

Purity:98.05%

Storage:Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month

Shipping:Room temperature in continental US; may vary elsewhere.

Description: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.

In Vitro: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].

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].

IC50 & Target:AMPK α1β1γ1 8.99 nM (EC50) AMPK α1β2γ1 126 nM (EC50) AMPK α2β1γ1 5.23 nM (EC50) AMPK α2β2γ1 42.2 nM (EC50)

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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.  [Content Brief]

Brand introduction:
•   MCE (MedChemExpress) has a global exclusive compound library of more than 200 kinds, and we are committed to providing the most comprehensive range of high-quality small molecule active compounds for scientific research customers around the world;
•   More than 50,000 highly selective inhibitors and agonists are involved in various popular signaling pathways and disease areas;
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•   The biological activity of the products has been verified by the experiments of customers in various countries;
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