MedKoo Biosciences, Inc.
Tel:   +1-919-636-5577    Fax:   +1-919-980-4831    Email:   sales@medkoo.com
Search
Login Register
Search
MedKoo Cat#: 530994 | Name: IOX4
Featured New

Description:

WARNING: This product is for research use only, not for human or veterinary use.

IOX4 is a potent inhibitor of PHD2 (IC50 = 1.6 nM). 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.

Chemical Structure

IOX4
IOX4
CAS#1154097-71-8

Theoretical Analysis

MedKoo Cat#: 530994

Name: IOX4

CAS#: 1154097-71-8

Chemical Formula: C15H16N6O3

Exact Mass: 328.1284

Molecular Weight: 328.33

Elemental Analysis: C, 54.87; H, 4.91; N, 25.60; O, 14.62

Price and Availability

Size Price Availability Quantity
100mg USD 950.00 2 Weeks
200mg USD 1,450.00 2 Weeks
500mg USD 2,950.00 2 Weeks
1g USD 3,950.00 2 Weeks
2g USD 6,950.00 2 Weeks
Bulk Inquiry
Buy Now
Add to Cart
Related CAS #
No Data
Synonym
IOX4; IOX-4; IOX 4.
IUPAC/Chemical Name
tert-butyl 6-(5-oxo-4-(1H-1,2,3-triazol-1-yl)-2,5-dihydro-1H-pyrazol-1-yl)nicotinate
InChi Key
HWQQDVNGHZIALS-UHFFFAOYSA-N
InChi Code
InChI=1S/C15H16N6O3/c1-15(2,3)24-14(23)10-4-5-12(16-8-10)21-13(22)11(9-18-21)20-7-6-17-19-20/h4-9,18H,1-3H3
SMILES Code
CC(C)(C)OC(C1=CN=C(N2NC=C(N3C=CN=N3)C2=O)C=C1)=O
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
Product Data
Product Data
Instruction
View handling instruction
Biological target:
IOX4 is a selective HIF prolyl-hydroxylase 2 (PHD2) inhibitor with an IC50 value of 1.6 nM, induces HIFα in cells and in wildtype mice with marked induction in the brain tissue. IOX4 competes with and displaces 2-oxoglutarate (2OG) at the active site of PHD2.
In vitro activity:
Induction of HIF1α levels were observed in MCF-7, Hep3B and U2OS cells treated with IOX2 and IOX4, with IOX4 apparently being markedly more potent than IOX2 (Fig 3D–3F). These cellular results are consistent with the in vitro data indicating that IOX4 is a substantially more potent PHD inhibitor than IOX2. Reference: PLoS One. 2015 Jul 6;10(7):e0132004. https://pubmed.ncbi.nlm.nih.gov/26147748/
In vivo activity:
Dose-dependent induction of both HIF1α and HIF2α in the liver and brain was observed after IOX4 treatment (Fig 4B and 4C). These observations reveal both IOX2 and IOX4 as active PHD inhibitors in mice; however, induction of HIF1α and HIF2α protein levels in the brain were only observed with IOX4. Reference: PLoS One. 2015 Jul 6;10(7):e0132004. https://pubmed.ncbi.nlm.nih.gov/26147748/
Solvent mg/mL mM
Solubility
DMF 25.0 76.14
DMF:PBS (pH 7.2) (1:1) 0.5 1.52
DMSO 45.3 138.07
Ethanol 2.0 6.09
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 328.33 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
1. Chan MC, Atasoylu O, Hodson E, Tumber A, Leung IK, Chowdhury R, Gómez-Pérez V, Demetriades M, Rydzik AM, Holt-Martyn J, Tian YM, Bishop T, Claridge TD, Kawamura A, Pugh CW, Ratcliffe PJ, Schofield CJ. Potent and Selective Triazole-Based Inhibitors of the Hypoxia-Inducible Factor Prolyl-Hydroxylases with Activity in the Murine Brain. PLoS One. 2015 Jul 6;10(7):e0132004. doi: 10.1371/journal.pone.0132004. PMID: 26147748; PMCID: PMC4492579.
In vitro protocol:
1. Chan MC, Atasoylu O, Hodson E, Tumber A, Leung IK, Chowdhury R, Gómez-Pérez V, Demetriades M, Rydzik AM, Holt-Martyn J, Tian YM, Bishop T, Claridge TD, Kawamura A, Pugh CW, Ratcliffe PJ, Schofield CJ. Potent and Selective Triazole-Based Inhibitors of the Hypoxia-Inducible Factor Prolyl-Hydroxylases with Activity in the Murine Brain. PLoS One. 2015 Jul 6;10(7):e0132004. doi: 10.1371/journal.pone.0132004. PMID: 26147748; PMCID: PMC4492579.
In vivo protocol:
1. Chan MC, Atasoylu O, Hodson E, Tumber A, Leung IK, Chowdhury R, Gómez-Pérez V, Demetriades M, Rydzik AM, Holt-Martyn J, Tian YM, Bishop T, Claridge TD, Kawamura A, Pugh CW, Ratcliffe PJ, Schofield CJ. Potent and Selective Triazole-Based Inhibitors of the Hypoxia-Inducible Factor Prolyl-Hydroxylases with Activity in the Murine Brain. PLoS One. 2015 Jul 6;10(7):e0132004. doi: 10.1371/journal.pone.0132004. PMID: 26147748; PMCID: PMC4492579.
1: Chan MC, Atasoylu O, Hodson E, Tumber A, Leung IK, Chowdhury R, Gómez-Pérez V, Demetriades M, Rydzik AM, Holt-Martyn J, Tian YM, Bishop T, Claridge TD, Kawamura A, Pugh CW, Ratcliffe PJ, Schofield CJ. Potent and Selective Triazole-Based Inhibitors of the Hypoxia-Inducible Factor Prolyl-Hydroxylases with Activity in the Murine Brain. PLoS One. 2015 Jul 6;10(7):e0132004. doi: 10.1371/journal.pone.0132004. eCollection 2015. PubMed PMID: 26147748; PubMed Central PMCID: PMC4492579.