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Biological Activity
HIF-prolyl hydroxylase-2 (PHD2) inhibitor. Blocks glutamate induced ROS production in HT-22 cells, independent of MnSOD. Exhibits neuroprotective effects and enhances functional recovery in rodent intracerebral hemorrhage models, via inhibition of ATF4 dependent genes. Brain penetrant. Also antioxidant.
Technical Data
| M. Wt | 377.82 |
| Formula | C21H16ClN3O2 |
| Storage | Store at -20°C |
| Purity | ≥97% (HPLC) |
| CAS Number | 385786-48-1 |
| PubChem ID | 3740671 |
| InChI Key | KKYHNYRUBSYTCZ-UHFFFAOYSA-N |
| Smiles | OC1=C(N=CC=C1)NC(C2=C(C3=C(C=C2)C=CC=N3)O)C4=CC=C(C=C4)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 | 37.78 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 377.82. 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 | 2.65 mL | 13.23 mL | 26.47 mL |
| 5 mM | 0.53 mL | 2.65 mL | 5.29 mL |
| 10 mM | 0.26 mL | 1.32 mL | 2.65 mL |
| 50 mM | 0.05 mL | 0.26 mL | 0.53 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Karuppagounder et al (2016) Therapeutic targeting of oxygen-sensing prolyl hydroxylases abrogates ATF4-dependent neuronal death and improves outcomes after brain hemorrhage in several rodent models. Sci.Transl.Med. 8 328ra29 PMID: 26936506
Neitemeier et al (2016) Inhibition of HIF-prolyl-4-hydroxylases prevents mitochondrial impairment and cell death in a model of neuronal oxytosis. Cell Death Dis. 7 e2214 PMID: 27148687
Keywords: Adaptaquin, supplier, HIF-PHD, inhibitors, hypoxia, inducible, factor, prolyl, hydroxylases, inhibits, antioxidant, neuroprotective, brain, penetrant., HIF, Hydroxylases, Hypoxia, Inducible, Factors, Hydroxylases, Tocris Bioscience
