Biological Activity
AMP-activated protein kinase (AMPK) activator (EC50 = 1 μM); activates AMPK indirectly through a CaMKKβ-dependent mechanism. Also inhibits LPS-induced STAT3 phosphorylation (IC50 = 0.5 μM). Induces autophagy and promotes Aβ degradation in vitro. Also inhibits adipogenesis in vitro and reduces weight gain in diet-induced obese mice.
Technical Data
| M. Wt | 312.37 |
| Formula | C17H20N4O2 |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 140405-36-3 |
| PubChem ID | 9613337 |
| InChI Key | GWQPCBPAOAFXSJ-XDHOZWIPSA-N |
| Smiles | O=C(N/N=C/C2=C(O)C=C(N(CC)CC)C=C2)C1=CC=NC=C1 |
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 | 15.62 | 50 | |
| ethanol | 1.56 | 5 |
Preparing Stock Solutions
The following data is based on the product molecular weight 312.37. 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 | 3.2 mL | 16.01 mL | 32.01 mL |
| 5 mM | 0.64 mL | 3.2 mL | 6.4 mL |
| 10 mM | 0.32 mL | 1.6 mL | 3.2 mL |
| 50 mM | 0.06 mL | 0.32 mL | 0.64 mL |
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References
References are publications that support the products' biological activity.
Vingtdeux et al (2011) Novel synthetic small-molecule activators of AMPK as enhancers of autophagy and amyloid-beta peptide degradation. FASEB J. 25 219 PMID: 20852062
Vingtdeux et al (2011) Small-molecule activators of AMP-activated protein kinase (AMPK), RSVA314 and RSVA405, inhibit adipogenesis. Mol Med 17 1022 PMID: 21647536
Capiralla et al (2012) Identification of potent small-molecule inhibitors of STAT3 with anti-inflammatory properties in RAW 264.7 macrophages. FASEB J. 279 3791 PMID: 22909341
Keywords: RSVA 405, supplier, RSVA405, AMP-activated, protein, kinases, activators, inhibitors, STAT3, indirect, Ab, Abeta, Aβ, amyloid, metabolism, nf-kb, nf-κb, cytokines, inhibits, AMPK, STAT, AMPK, Tocris Bioscience
