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PZ0319

Sigma-Aldrich

PF-06409577

≥98% (HPLC)

Synonym(e):

6-Chloro-5-[4-(1-hydroxycyclobutyl)phenyl]-1H-indole-3-carboxylic acid

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About This Item

Empirische Formel (Hill-System):
C19H16ClNO3
CAS-Nummer:
1467057-23-3
Molekulargewicht:
341.79
UNSPSC-Code:
12352200
PubChem Substanz-ID:
329823837
NACRES:
NA.77

Qualitätsniveau

100

Assay

≥98% (HPLC)

Form

powder

Farbe

white to beige

Löslichkeit

DMSO: 20 mg/mL, clear

Lagertemp.

room temp

SMILES String

ClC1=C(C2=CC=C(C3(O)CCC3)C=C2)C=C4C(NC=C4C(O)=O)=C1

InChI

1S/C19H16ClNO3/c20-16-9-17-14(15(10-21-17)18(22)23)8-13(16)11-2-4-12(5-3-11)19(24)6-1-7-19/h2-5,8-10,21,24H,1,6-7H2,(H,22,23)

InChIKey

FHQXLWCFSUSXBF-UHFFFAOYSA-N

Allgemeine Beschreibung

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

Anwendung

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

Biochem./physiol. Wirkung

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

Piktogramme

Exclamation mark
GHS07

Signalwort

Warning

Gefahreneinstufungen

Eye Irrit. 2 - Skin Irrit. 2 - STOT SE 3

Zielorgane

Respiratory system

Lagerklassenschlüssel

11 - Combustible Solids

WGK

WGK 3

Flammpunkt (°F)

Not applicable

Flammpunkt (°C)

Not applicable

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Analysenzertifikate (COA)

Lot/Batch Number
026M4742V

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Die Dokumentenbibliothek aufrufen

Nereida Jiménez de Oya et al.
Antimicrobial agents and chemotherapy, 62(7) (2018-05-02)
Mosquito-borne flaviviruses are a group of RNA viruses that constitute global threats for human and animal health. Replication of these pathogens is strictly dependent on cellular lipid metabolism. We have evaluated the effect of the pharmacological activation of AMP-activated protein
Discovery and Preclinical Characterization of 6-Chloro-5-[4-(1-hydroxycyclobutyl)phenyl]-1H-indole-3-carboxylic Acid (PF-06409577), a Direct Activator of Adenosine Monophosphate-activated Protein Kinase (AMPK), for the Potential Treatment of Diabetic Nephropathy.
Cameron KO et al
Journal of Medicinal Chemistry, 59(17), 8068-8081 (2016)
PF-06409577 activates AMPK signaling to protect retinal pigment epithelium cells from UV radiation.
Li X F, et al.
Biochemical and Biophysical Research Communications, 501(1), 293-299 (2018)
Activation of Liver AMPK with PF-06409577 Corrects NAFLD and Lowers Cholesterol in Rodent and Primate Preclinical Models.
Esquejo RM, et al.
EBioMedicine, 31, 122-132 (2018)

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