IOX4

Base Information

• Chemical Name: IOX4
• CAS No.: 1154097-71-8
• Molecular Formula: C₁₅H₁₆N₆O₃
• Molecular Weight: 328.33
• Mol file: 1154097-71-8.mol

Synonyms:

Chemical Property of IOX4

Chemical Property:

• Melting Point: >190° (dec.)
• Boiling Point: 502.2±60.0 °C(Predicted)
• PKA: 1.36±0.29(Predicted)
• Density: 1.41±0.1 g/cm3(Predicted)
• Storage Temp.: Refrigerator, Under inert atmosphere
• Solubility.: DMSO (Sparingly, Sonicated), Methanol (Slightly, Sonicated)

Purity/Quality:

99%+, ^*data from raw suppliers

IOX4 ^*data from reagent suppliers

Safty Information:

• Pictogram(s):  
• Hazard Codes: 

MSDS Files:

Useful:

• 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.

Technology Process of IOX4

There total 1 articles about IOX4 which guide to synthetic route it. The literature collected by LookChem mainly comes from the sharing of users and the free literature resources found by Internet computing technology. We keep the original model of the professional version of literature to make it easier and faster for users to retrieve and use. At the same time, we analyze and calculate the most feasible synthesis route with the highest yield for your reference as below:

synthetic route:

Reference yield: 29.0%

DMF + t-butyl-6-hydrazinylnicotinate + ethyl 2-(1H-1,2,3-triazol-1-yl)acetate (4314-21-0) → t-butyl 6-(5-oxo-4-(1H-1,2,3-triazol-1-yl)-2,5-dihydro-1H-pyrazol-1-yl)nicotinate (1154097-71-8)

Guidance literature:

t-butyl-6-hydrazinylnicotinate; In ethanol; at 20 ℃;

DMF; ethyl 2-(1H-1,2,3-triazol-1-yl)acetate; In ethanol; at 20 ℃; Sealed tube;

In ethanol; trifluoroacetic acid; at 80 ℃; for 12h; Sealed tube;

DOI:10.1371/journal.pone.0132004

upstream raw materials:

ethyl 2-(1H-1,2,3-triazol-1-yl)acetate

Refernces