PF-06409577

Catalog No.S8335

PF-06409577 Chemical Structure

Molecular Weight(MW): 341.79

PF-06409577 is 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.

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Biological Activity

Description PF-06409577 is 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

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 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].

Protocol

Animal Research:

[2]

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  • Animal Models: ZSF-1 rats
  • Formulation: 5% Vitamin E TPGS in water
  • Dosages: 100 mg/kg
  • Administration: by oral gavage
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 68 mg/mL (198.95 mM)
Ethanol 68 mg/mL (198.95 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 341.79
Formula

C19H16ClNO3

CAS No. 1467057-23-3
Storage powder
in solvent
Synonyms N/A

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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.

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AMPK Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID