Basic information Safety Supplier Related

6-chloro-5-(4-(1-hydroxycyclobutyl)phenyl)-1H-indole-3-carboxylicacid

Basic information Safety Supplier Related

6-chloro-5-(4-(1-hydroxycyclobutyl)phenyl)-1H-indole-3-carboxylicacid Basic information

Product Name:
6-chloro-5-(4-(1-hydroxycyclobutyl)phenyl)-1H-indole-3-carboxylicacid
Synonyms:
  • CS-2760
  • PF-06409577;PF 06409577;PF06409577
  • 6-chloro-5-(4-(1-hydroxycyclobutyl)phenyl)-1H-indole-3-carboxylicacid
  • PF-06409577
  • EOS-61684
  • PF 06409577;PF06409577
  • PF 6409577
  • 1H-Indole-3-carboxylic acid, 6-chloro-5-[4-(1-hydroxycyclobutyl)phenyl]-
CAS:
1467057-23-3
MF:
C19H16ClNO3
MW:
341.79
Mol File:
1467057-23-3.mol
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6-chloro-5-(4-(1-hydroxycyclobutyl)phenyl)-1H-indole-3-carboxylicacid Chemical Properties

Boiling point:
610.9±55.0 °C(Predicted)
Density 
1.468±0.06 g/cm3(Predicted)
storage temp. 
room temp
solubility 
DMSO: soluble
form 
powder
pka
3.60±0.30(Predicted)
color 
white to beige
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6-chloro-5-(4-(1-hydroxycyclobutyl)phenyl)-1H-indole-3-carboxylicacid Usage And Synthesis

Description

PF-06409577 is an activator of AMP-activated protein kinase (AMPK) heterotrimers (Kd = 9 nM for α1β1γ1). In vitro, it selectively activates β1-containing AMPK isoforms (EC50s = 2.18-7.03 nM) over β2-containing isoforms (EC50s = ≥10 μM). PF-06409577 has an EC50 value of 7 nM in an activation/protection TR-FRET assay using α1β1γ1 AMPK. In vivo, PF-06409577 (≥10 mg/kg) increases phosphorylation of AMPK in rat kidney. It decreases urinary albumin levels in a ZSF1 obese rat model of diabetes, metabolic syndrome, and renal disease when administered at a dose of 100 mg/kg.

Uses

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

General Description

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

Biochem/physiol Actions

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.

storage

Store at RT

6-chloro-5-(4-(1-hydroxycyclobutyl)phenyl)-1H-indole-3-carboxylicacidSupplier

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