IOX4 | CAS#1154097-71-8 | PHD2 inhibitor

IOX4
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WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 530994

CAS#: 1154097-71-8

Description: 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

CAS# 1154097-71-8

Product data Instruction

Theoretical Analysis

MedKoo Cat#: 530994
Name: IOX4
CAS#: 1154097-71-8
Chemical Formula: C15H16N6O3
Exact Mass: 328.13
Molecular Weight: 328.332
Elemental Analysis: C, 54.87; H, 4.91; N, 25.60; O, 14.62

Price and Availability

Size	Price	Availability
100mg	USD 950	2 Weeks
200mg	USD 1450	2 Weeks
500mg	USD 2950	2 Weeks
1g	USD 3950	2 Weeks
2g	USD 6950	2 Weeks
Bulk inquiry Welcome, Customer: Please do not inquire quote if your intended use is for a patient since our products are for research use and for chemical synthesis use, not for human use . For in-stock products, we listed price in the web page. You may inquire prices for which sizes were not listed. If no price is listed, this means the product is not in stock at the moment, which may be available via custom synthesis. For cost-effective reason, minimum order of 1g is requested (typically very expensive). The lead time is usually 2-4 months. Quote of less than 1g will not be provided. MedKoo may not offer quote for below reasons: (1) current available synthetic method appears to be extremely expensive which is obviously not affordable to most customers; (2) Key raw material to make the product is temporally not available; (3) DEA controlled substances; (4) the product is under patent protection in customer’s country.

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:

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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/

Solubility Data

	Solvent	Max Conc. mg/mL	Max Conc. 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

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.

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.

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*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / CoA (available online).

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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.

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