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