Biological Activity
HIF pathway activator (EC50 values are 1.23 and 1.4 μM for HRE gene reporter assay and HIF-1α nuclear translocation assay respectively); acts via chelation of iron, independently of PHD. Also exhibits > 80% inhibition of the human A3 receptor, dopamine transporter, μ receptor, hERG and 5-HT2B receptor, and rat sodium channel site 2, at a concentration of 10 μM.
Compound Libraries
ML 228 is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 415.49 |
| Formula | C27H21N5 |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 1357171-62-0 |
| PubChem ID | 46742353 |
| InChI Key | QNRODODTMXCRKU-UHFFFAOYSA-N |
| Smiles | C1(C2=NC(NCC4=CC=C(C5=CC=CC=C5)C=C4)=C(C3=CC=CC=C3)N=N2)=NC=CC=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 | 41.55 | 100 | |
| ethanol | 8.31 | 20 |
Preparing Stock Solutions
The following data is based on the product molecular weight 415.49. 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 | 2.41 mL | 12.03 mL | 24.07 mL |
| 5 mM | 0.48 mL | 2.41 mL | 4.81 mL |
| 10 mM | 0.24 mL | 1.2 mL | 2.41 mL |
| 50 mM | 0.05 mL | 0.24 mL | 0.48 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Theriault et al (2012) Discovery of a new molecular probe ML228: an activator of the hypoxia inducible factor (HIF) pathway. Bioorg.Med.Chem.Lett. 22 76 PMID: 22172704
Keywords: ML 228, supplier, ML228, hypoxia, inducible, factor, HIF, pathway, activators, iron, chelators, HRE, HIF, Hypoxia, Inducible, Factors, HIF, Tocris Bioscience
