Biological Activity
Potent and selective allosteric activator of AMPK (EC50 values are 7 and >40000 nM for AMPKα1β1γ1 and AMPKα1β2γ1, respectively). Exhibits minimal off-target effects on a panel of receptors, ion channels, PDEs and kinases. Improves kidney function and reduces proteinuria in a preclinical model of diabetic nephropathy. Orally bioavailable.
Licensing Information
Sold for research purposes under agreement from Pfizer Inc.
Technical Data
| M. Wt | 341.79 |
| Formula | C19H16ClNO3 |
| Storage | Store at RT |
| Purity | ≥98% (HPLC) |
| CAS Number | 1467057-23-3 |
| PubChem ID | 71748255 |
| InChI Key | FHQXLWCFSUSXBF-UHFFFAOYSA-N |
| Smiles | O=C(O)C1=CNC2=CC(Cl)=C(C3=CC=C(C4(CCC4)O)C=C3)C=C21 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 34.18 | 100 | |
| ethanol | 6.84 | 20 |
Preparing Stock Solutions
The following data is based on the product molecular weight 341.79. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.93 mL | 14.63 mL | 29.26 mL |
| 5 mM | 0.59 mL | 2.93 mL | 5.85 mL |
| 10 mM | 0.29 mL | 1.46 mL | 2.93 mL |
| 50 mM | 0.06 mL | 0.29 mL | 0.59 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Cameron et al (2016) 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 diab J.Med.Chem. 59 8068 PMID: 27490827
Salatto et al (2017) Selective activation of AMPK β1-containing isoforms improves kidney function in a rat model of diabetic nephropathy. J.Pharmacol.Exp.Ther. 361 303 PMID: 28289077
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