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PF-06409577

Catalog No. T4427 CAS 1467057-23-3

Synonyms: PF 06409577

PF-06409577 is an effective, orally active, and specific allosteric activator of AMPK (EC50: 7 nM, for α1β1γ1).

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PF-06409577, CAS 1467057-23-3

Pack Size	Availability	Price/USD
2 mg	In stock	$ 38.00
5 mg	In stock	$ 61.00
10 mg	In stock	$ 107.00
25 mg	In stock	$ 222.00
50 mg	In stock	$ 402.00
100 mg	In stock	$ 598.00
500 mg	In stock	$ 1,290.00
1 mL * 10 mM (in DMSO)	In stock	$ 68.00

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Purity: 98.16%

Purity: 95.17%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	PF-06409577 is an effective, orally active, and specific allosteric activator of AMPK (EC50: 7 nM, for α1β1γ1).
Targets&IC50	AMPK α1β1γ1:7 nM (EC50)
In vitro	In human and rat , PF-06409577 has similar effectiveness for α1β1γ1 isoforms. PF-06409577 exhibits minimal off-target effects on a panel of receptors, ion channels, PDEs, and kinases. PF-06409577 has no inhibition of hERG in a patch-clamp assay (100 μM) and is not an inhibitor (IC50>100 μM) of the microsomal activities of major human cytochrome P450 isoforms[1].
In vivo	In rats, monkeys, and dogs, PF-06409577 has moderate plasma clearance and is well distributed with steady-state distribution volume. Following oral administration of crystalline PF-06409577 in 0.5% methylcellulose suspension, PF-06409577 is rapidly absorbed in dogs, rats, and monkeys. The corresponding oral bioavailability values in rats, monkeys, and dogs are 15%, 59%, and 100%, respectively. Dose-dependent increases in pAMPK relative to total AMPK (tAMPK) in whole kidney tissue are observed with a maximal 3.8-fold response at 300 mg/kg PF-06409577 treatment[1]. Oral administration of PF-06409577 (10, 30, and 100 mg/kg every day) resulted in dose-dependent reductions in proteinuria in the obese ZSF1 animals, with greater than 2-fold reduction in 24-hour urinary albumin loss compared with vehicle control after 60 days of treatment [2].
Kinase Assay	PF-06409577 is prepared in DMSO. PF-06409577 is incubated with fully phosphorylated AMPK in assay buffer at room temperature for 15 min followed by addition of PP2a and another incubation for 60 min at room temperature. The phosphatase treatment is quenched and the kinase assay initiated with the addition of okadaic acid (50 nM final), 50 nM Cy-5 SAMS peptide and ATP equal to Km for each isoform. Reactions are incubated for an additional 60 min and the kinase reaction is quenched with the addition of 10 mM EDTA and 2 nM Eu-pACC antibody in detection Buffer. Kinase activity is monitored by excitation at 320 nM and measuring emission at 665 and 615 nM, respectively[2].
Animal Research	PF-06409577 is prepared in 0.5% methylcellulose[2].Daily administration of 0.5% methylcellulose (p.o.), PF-06409577 at 10, 30, or 100 mg/kg (p.o.), PF- 249 at 3, 10, or 30 mg/kg (p.o.), or ramipril in drinking water (1 mg/kg/day) is initiated and continued for 68 days. Urine is collected for 24-hours and volume recorded from all lean and obese rats after 14, 28, 42, and 60 days of dosing. On Day 63 all rats are administered a final dose after 16-hour overnight fasting. One hour following the final dose, blood glucose is measured by glucometer and a 100 μL tail vein blood sample collected and processed for determination of insulin levels and total protein. Each rat is then anesthetized with isoflurane. The right kidney is collected and immediately freeze-clamped and transferred to liquid nitrogen storage; the left kidney is fixed in 10% formalin. Rats are then euthanized by exsanguination from the vena cava[2].

Synonyms	PF 06409577
Molecular Weight	341.79
Formula	C19H16ClNO3
CAS No.	1467057-23-3

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: 6.8 mg/mL(20 mM)

DMSO: 34.2 mg/mL(100 mM)

H2O: Insoluble

References and Literature

1. Cameron K O, Kung D W, Kalgutkar A S, et al. Discovery and preClinicalal characterization of 6-chloro-5-[4-(1-hydroxycyclobutyl) phenyl]-1 H-indole-3-carboxylic Acid (PF-06409577), a direct activator of adenosine monophosphate-activated protein kinase (AMPK), for the potential treatment of diabetic nephropathy[J]. Journal of medicinal chemistry, 2016, 59(17): 8068-8081. 2. Salatto C T, Miller R A, Cameron K O, et al. Selective activation of AMPK β1-containing isoforms improves kidney function in a rat model of diabetic nephropathy[J]. Journal of Pharmacology and Experimental Therapeutics, 2017, 361(2): 303-311.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Clinical Compound Library Anti-Cancer Drug Library Kinase Inhibitor Library Drug Repurposing Compound Library Bioactive Compound Library Lipid Metabolism Compound Library Anti-Pancreatic Cancer Compound Library Reprogramming Compound Library ReFRAME Related Library Anti-Diabetic Compound Library

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Keywords

PF-06409577 1467057-23-3 Chromatin/Epigenetic PI3K/Akt/mTOR signaling AMPK Inhibitor AMP-activated protein kinase inhibit PF 06409577 PF06409577 inhibitor

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