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| Product Name: | IOX4 | | Synonyms: | IOX4;tert-butyl 6-(5-oxo-4-(1H-1,2,3-triazol-1-yl)-2,5-dihydro-1H-pyrazol-1-yl)nicotinate;3-Pyridinecarboxylic acid, 6-[2,5-dihydro-5-oxo-4-(1H-1,2,3-triazol-1-yl)-1H-pyrazol-1-yl]-, 1,1-dimethylethyl ester;t-butyl 6-(5-oxo-4-(1H-1,2,3-triazol-1-yl)-2,5-dihydro-1H-pyrazol-1-yl)nicotinate;IOX4; IOX-4; IOX 4;PHD2 inhibitor IOX4;IOX4 NEW;IOX 4,HIF-PH,HIFs,Hypoxia-inducible factors,IOX4,IOX-4,inhibit,HIF/HIF Prolyl-Hydroxylase,Inhibitor | | CAS: | 1154097-71-8 | | MF: | C15H16N6O3 | | MW: | 328.33 | | EINECS: | | | Product Categories: | | | Mol File: | 1154097-71-8.mol |  |
| Melting point | >190° (dec.) | | Boiling point | 502.2±60.0 °C(Predicted) | | density | 1.41±0.1 g/cm3(Predicted) | | storage temp. | Refrigerator, Under inert atmosphere | | solubility | DMSO (Sparingly, Sonicated), Methanol (Slightly, Sonicated) | | form | Solid | | pka | 1.36±0.29(Predicted) | | color | Light Beige to Beige |
| Description | IOX4 is a potent inhibitor of hypoxia-inducible factor prolyl hydroxylase 2 (HIF-PH2; IC50 = 1.6 nM). It displays >1,000-fold selectivity for PHD2 over other 2OG-dependent dioxygenases, including JMJD isoforms, FBXL11, JARID1C, BBOX1, FIH, and FTO. IOX4 is active in vivo, inhibiting prolyl hydroxylation and increasing HIF-1α levels in cells (IC50 values range from 5.6 to 11.7 μM) and inducing HIF-1α and HIF-2α expression in mice. The induction of HIF expression in mice occurs in the brain as well as in the liver, kidney, and heart, indicating that IOX4 penetrates the blood-brain barrier. | | Uses | IOX4 is a triazole based potent and selective inhibitor of hypoxia-inducible factor (HIF) prolyl-hydroxylase. It induces HIFα in cells of mouse brain. It is useful for studies that aim to validate the upregulation of HIF for treatment of cerebral diseases such as stroke. |
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