Home PI3K/Akt/mTOR AMPK activator PF-06409577 For research use only.

PF-06409577

PF-06409577 is an orally bioavailable AMPK activator with EC50 of 7 nM for α1β1γ1 in the TR-FRET assay and it shows no detectable inhibition of hERG in a patch-clamp assay (100 μM) and was not an inhibitor (IC50 > 100 μM) of the microsomal activities of major human cytochrome P450 isoforms.

PF-06409577 Chemical Structure

PF-06409577 Chemical Structure

CAS No. 1467057-23-3

Purity & Quality Control

Batch: S833501 DMSO]68 mg/mL]false]Ethanol]68 mg/mL]false]Water]Insoluble]false Purity: 99.44%
99.44

PF-06409577 Related Products

Signaling Pathway

AMPK Signaling Pathways

AMPK Signaling Pathway

Biological Activity

Description PF-06409577 is an orally bioavailable AMPK activator with EC50 of 7 nM for α1β1γ1 in the TR-FRET assay and it shows no detectable inhibition of hERG in a patch-clamp assay (100 μM) and was not an inhibitor (IC50 > 100 μM) of the microsomal activities of major human cytochrome P450 isoforms.
Targets
AMPK α2β1γ1 [1] AMPK α1β1γ1 [1]
6.8 nM(EC50) 7 nM(EC50)
In vitro
In vitro PF-06409577 activates α1β1γ1 and α2β1γ1 AMPK isoforms with EC50 of 7.0 nM and 6.8 nM but was much less active against α1β2γ1/α2β2γ1/α2β2γ3 AMPK isoforms with EC50 greater 4000 nM[1].
In Vivo
In vivo PF-06409577 exhibits efficacy in a preclinical model of diabetic nephropathy[1]. It exhibits high plasma protein binding in rat (plasma unbound fraction, fu,p = 0.0044), dog (fu,p = 0.028), monkey (fu,p = 0.032), and human (fu,p = 0.017). Following iv administration, PF-06409577 demonstrates moderate plasma clearance (CLp) in rats (22.6 mL/min/kg), dogs (12.9 mL/min/kg), and monkeys (8.57 mL/min/kg) and was well distributed with steady state distribution volumes (Vdss) ranging from 0.846-3.15 L/kg. Following oral administration of crystalline PF-06409577 in 0.5% methylcellulose suspension, PF-06409577 is rapidly absorbed (Tmax = 0.25-1.20 h) in rats, dogs, and monkeys. The corresponding oral bioavailability (F) values in rats, dogs, and monkeys, were 15%, 100%, and 59%, respectively. PF-06409577 is subject to a higher degree of first pass intestinal glucuronidation in the rat (relative to other preclinical species and human)[2].
Animal Research Animal Models ZSF-1 rats
Dosages 100 mg/kg
Administration by oral gavage
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02286882 Terminated
Healthy
Pfizer
 November 2014 Phase 1

Chemical Information & Solubility

Molecular Weight 341.79 Formula

C19H16ClNO3
CAS No. 1467057-23-3 SDF Download PF-06409577 SDF
Smiles C1CC(C1)(C2=CC=C(C=C2)C3=C(C=C4C(=C3)C(=CN4)C(=O)O)Cl)O
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 68 mg/mL ( (198.95 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 68 mg/mL

Water : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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