Application

PF-06409577 has been used to determine its potential as a therapeutic agent for diabetic nephropathy.

Biochem/physiol Actions

PF-06409577 potently activates a1β1γ1 AMPK (5′ adenosine monophosphate-activated protein kinase) isoform, and prevents its dephosphorylation. It is similarly potent for β1 containing isoforms, but shows significantly lower potency for β2-containing isoforms of AMPK. Patch-clamp assays show that this compound does not inhibit hERG (human ether-a-go-go gene). It interacts with the allosteric drug and metabolite site (ADaM) of AMPK.

PF-06409577 preserves retinal pigment epithelium cells from UV radiation by activating AMPK (AMP-activated protein kinase) signaling. This orally bioavailable and possesses pharmacokinetic properties. PF-06409577 blocks de novo lipid and cholesterol synthesis pathways that shows a decrease in hepatic lipids and mRNA expression of markers of hepatic fibrosis.

PF-06409577 is a potent and selective activator of 5′ adenosine monophosphate-activated protein kinase (AMPK).

General description

PF-06409577 is a 6-chloro-indole derivative obtained from 5-bromo-6-chloro-indole.

Legal Information

Pfizer is a registered trademark of Pfizer, Inc.

Sold for research purposes under agreement from Pfizer Inc.

Other Notes

This compound was developed by Pfizer for Kinase Phosphatase Biology research. To learn more about Sigma′s partnership with Pfizer and view other authentic, high-quality Pfizer compounds, visit sigma.com/bsm-pfizer.

Packaging

5, 25 mg in glass bottle