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PF-06685249

Chemical Structure : PF-06685249

CAS No.: 1467059-70-6

PF-06685249 (PF06685249, PF-249)

Catalog No.: PC-62774Not For Human Use, Lab Use Only.

PF-06685249 (PF06685249, PF-249) is a novel potent, orally active, α1β1γ1/α2β1γ1-isoform selective AMPK activator with Kd of 14 nM, EC50 of 12 nM for α1β1γ1-AMPK.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

PF-06685249 (PF06685249, PF-249) is a novel potent, orally active, α1β1γ1/α2β1γ1-isoform selective AMPK activator with Kd of 14 nM, EC50 of 12 nM for α1β1γ1-AMPK.
PF-06685249 (PF06685249, PF-249) shows minimal activity at the β2-containing isoforms (α1β2γ1, α2β2γ1, α2β2γ3).
PF-06685249 (PF06685249, PF-249) demonstrates in vivo target engagement experiment in ZSF-1 rats, an obese/diabetic rodent model of diabetic nephropathy.

Physicochemical Properties

M.Wt 345.783
Formula C17H16ClN3O3
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

6-Chloro-5-(6-(dimethylamino)-2-methoxypyridin-3-yl)-1H-indole-3-carboxylic acid

References

1. Edmonds DJ, et al. J Med Chem. 2018 Feb 28. doi: 10.1021/acs.jmedchem.7b01641.

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