Biological Activity
Allosteric AMP-activated protein kinase (AMPK) activator; allosterically stimulates active AMPK heterotrimers, increasing the activity of α1β1γ1 by 1.5-fold and α2β1γ1 by 1.7-fold (EC50 values are 0.42 and 0.95 μM, respectively). Inhibits dephosphorylation of AMPK Thr-172 by PP2Cα. Stimulates glucose uptake and fatty acid oxidation without increasing the ADP/ATP ratio. Also decreases fatty acid synthesis and glucose output in primary hepatocytes. Improves glucose tolerance and decreases cholesterol content in db/db mice.
Compound Libraries
ZLN 024 hydrochloride is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 361.69 |
| Formula | C13H13BrN2OS.HCl |
| Storage | Store at +4°C |
| Purity | ≥99% (HPLC) |
| PubChem ID | 91654626 |
| InChI Key | MMQCYIMDROWWFE-UHFFFAOYSA-N |
| Smiles | BrC1=C(OCCSC2=NC=CC=N2)C=CC(C)=C1.Cl |
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 | 36.17 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 361.69. 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 | 2.76 mL | 13.82 mL | 27.65 mL |
| 5 mM | 0.55 mL | 2.76 mL | 5.53 mL |
| 10 mM | 0.28 mL | 1.38 mL | 2.76 mL |
| 50 mM | 0.06 mL | 0.28 mL | 0.55 mL |
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References
References are publications that support the products' biological activity.
Li et al (2013) Novel small-molecule AMPK activator orally exerts beneficial effects on diabetic db/db mice. Toxicol.Appl.Pharmacol. 273 325 PMID: 24055643
Zhang et al (2013) Novel small-molecule AMP-activated protein kinase allosteric activator with beneficial effects in db/db mice. PLoS One 8 e72092 PMID: 23977216
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