An activator of AMPK heterotrimers (Kd = 9 nM for α1β1γ1); selectively activates β1-containing AMPK isoforms (EC50s = 2.18-7.03 nM) over β2-containing isoforms (EC50s = ≥10 μM); EC50 = 7 nM in an activation/protection TR-FRET assay using α1β1γ1 AMPK; increases phosphorylation of AMPK in rat kidney in vivo at ≥10 mg/kg; decreases urinary albumin levels in a ZSF1 obese rat model of diabetes

PF-06409577 – 10 mg

Brand:
Cayman
CAS:
1467057-23-3
Storage:
-20
UN-No:
Non-Hazardous - /

PF-06409577 is an activator of AMP-activated protein kinase (AMPK) heterotrimers (Kd = 9 nM for α1β1γ1).{47255} 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.  

 

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SKU: 27366 - 10 mg Category:

Description

An activator of AMPK heterotrimers (Kd = 9 nM for α1β1γ1); selectively activates β1-containing AMPK isoforms (EC50s = 2.18-7.03 nM) over β2-containing isoforms (EC50s = ≥10 μM); EC50 = 7 nM in an activation/protection TR-FRET assay using α1β1γ1 AMPK; increases phosphorylation of AMPK in rat kidney in vivo at ≥10 mg/kg; decreases urinary albumin levels in a ZSF1 obese rat model of diabetes, metabolic syndrome, and renal disease at 100 mg/kg

Formal name: 6-chloro-5-[4-(1-hydroxycyclobutyl)phenyl]-1H-indole-3-carboxylic acid

Synonyms: 

Molecular weight: 341.8

CAS: 1467057-23-3

Purity: ≥98%

Formulation: A solid

Product Type|Biochemicals|Small Molecule Activators|Kinases||Research Area|Cardiovascular System|Kidney & Renal Disease|Diabetic Nephropathy||Research Area|Endocrinology & Metabolism|Metabolic Diseases|Diabetes||Research Area|Endocrinology & Metabolism|Metabolic Diseases|Metabolic Syndrome

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