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IOX4

Cat. No. M11006
IOX4  Structure
Size Price Availability Quantity
5mg USD 60  USD60 In stock
10mg USD 105  USD105 In stock
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Quality Control & Documentation
Biological Activity

IOX4 is a selective PHD2 inhibitor,IC50 With a value of 1.6 nM, HIFα expression is induced in cells and wild-type mice to permeate the blood-brain barrier. IOX4 competes with and displaces 2-oxoglutaric acid (2OG) at the PHD2 active site.

Chemical Information
Molecular Weight 328.33
Formula C15H16N6O3
CAS Number 1154097-71-8
Solubility (25°C) DMSO ≥ 60 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Hideaki Ishii, et al. Drug Test Anal. Long-term monitoring of IOX4 in horse hair and its longitudinal distribution with segmental analysis using liquid chromatography/electrospray ionization Q Exactive high-resolution mass spectrometry for the purpose of doping control

[2] Hideaki Ishii, et al. Drug Test Anal. Comprehensive metabolic study of IOX4 in equine urine and plasma using liquid chromatography/electrospray ionization Q Exactive high-resolution mass spectrometer for the purpose of doping control

[3] William D Figg Jr, et al. ChemMedChem. Structural Basis of Prolyl Hydroxylase Domain Inhibition by Molidustat

[4] Moses Philip, et al. Drug Test Anal. Metabolic studies of hypoxia-inducible factor stabilisers IOX2, IOX3 and IOX4 (in vitro) for doping control

[5] Monica Mazzarino, et al. J Anal Toxicol. UPLC-MS-Based Procedures to Detect Prolyl-Hydroxylase Inhibitors of HIF in Urine

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HIV-IN-7

Axl-IN-16 is a Axl inhibitor.

HIF-2α-IN-9

HIF-2α-IN-9 is an inhibitor ofHIF-2α.

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PHD-IN-2 is a PHD antagonist (IC50: < 5 nM).

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Keywords: IOX4 supplier, HIF, inhibitors, activators


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