1154097-71-8

Usage

Uses

Used in Pharmaceutical Research:
IOX4 is used as a research tool for validating the upregulation of HIF in the treatment of cerebral diseases such as stroke. Its ability to induce HIFα in cells of the mouse brain makes it a valuable compound for studying the potential therapeutic effects of HIF modulation in various conditions.
Used in Drug Development:
IOX4 is utilized in the development of drugs targeting hypoxia-inducible factor prolyl hydroxylase, with potential applications in treating cerebral diseases and other conditions where HIF regulation may play a crucial role. Its high selectivity and in vivo activity make it a promising candidate for further research and development in the pharmaceutical industry.

Upstream product

• 4314-21-0 ethyl 2-(1H-1,2,3-triazol-1-yl)acetate 

Relevant academic research and scientific papers

Potent and selective triazole-based inhibitors of the hypoxia-inducible factor prolyl-hydroxylases with activity in the murine brain

As part of the cellular adaptation to limiting oxygen availability in animals, the expression of a large set of genes is activated by the upregulation of the hypoxia-inducible transcription factors (HIFs). Therapeutic activation of the natural human hypoxic response can be achieved by the inhibition of the hypoxia sensors for the HIF system, i.e. the HIF prolylhydroxylases (PHDs). Here, we report studies on tricyclic triazole-containing compounds as potent and selective PHD inhibitors which compete with the 2-oxoglutarate co-substrate. One compound (IOX4) induces HIFα in cells and in wildtype mice with marked induction in the brain tissue, revealing that it is useful for studies aimed at validating the upregulation of HIF for treatment of cerebral diseases including stroke.