ML228 | CAS#1357171-62-0 | HIF pathway activator

MedKoo Cat#: 462573 | Name: ML228

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Description:

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

ML228 is a potent the Hypoxia Inducible Factor (HIF) pathway activator. It potently activates HIF in vitro as well as its downstream target VEGF.

Chemical Structure

ML228

CAS#1357171-62-0

Theoretical Analysis

MedKoo Cat#: 462573

Name: ML228

CAS#: 1357171-62-0

Chemical Formula: C27H21N5

Exact Mass: 415.1797

Molecular Weight: 415.50

Elemental Analysis: C, 78.05; H, 5.09; N, 16.86

Price and Availability

Size	Price	Availability
5mg	USD 310.00	2 Weeks
10mg	USD 500.00	2 Weeks
50mg	USD 1,310.00	2 Weeks

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Related CAS #

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Synonym

ML228; CID-46742353

IUPAC/Chemical Name

N-([1,1'-biphenyl]-4-ylmethyl)-6-phenyl-3-(pyridin-2-yl)-1,2,4-triazin-5-amine

InChi Key

QNRODODTMXCRKU-UHFFFAOYSA-N

InChi Code

InChI=1S/C27H21N5/c1-3-9-21(10-4-1)22-16-14-20(15-17-22)19-29-27-25(23-11-5-2-6-12-23)31-32-26(30-27)24-13-7-8-18-28-24/h1-18H,19H2,(H,29,30,32)

SMILES Code

C1(C2=NC=CC=C2)=NC(NCC3=CC=C(C4=CC=CC=C4)C=C3)=C(C5=CC=CC=C5)N=N1

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

>3 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:

ML228 (CID-46742353) is a potent the Hypoxia Inducible Factor (HIF) pathway activator with EC50 of 1 μM.

In vitro activity:

The probe compound ML228 was among the top active compounds in each of the three HIF-specific activity assays and was inactive in the proteasome inhibition counterscreen assay (Figure 3). ML228 was found to inhibit greater than 75% of radioligand binding in six assays when tested at a concentration of 10 μM (Table 5). Reference: Bioorg Med Chem Lett. 2012 Jan 1;22(1):76-81. https://pubmed.ncbi.nlm.nih.gov/22172704/

In vivo activity:

A total of 90 12-week-old Sprague Dawley rats were randomly divided into the following three groups: Sham group (operation without SCI (spinal cord injury)); control group (SCI without ML228 treatment); and treatment group (SCI receiving ML228 treatment). The results of the current study suggest that ML228 may effectively activate the HIF-1α/VEGF signaling pathway to promote the expression of HIF-1α and VEGF proteins within the injured segment of the spinal cord, which promotes neural functional recovery following SCI in rats. Therefore, treatment with ML228 may be developed as a novel therapeutic strategy to treat SCI. Reference: Exp Ther Med. 2017 Mar;13(3):861-866. https://pubmed.ncbi.nlm.nih.gov/28450910/

	Solvent	mg/mL	mM
Solubility
	DMSO	30.0	72.20
	Ethanol	30.0	72.20
	Ethanol:PBS (pH 7.2) (1:2)	0.3	0.60

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 415.50 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. Zhu D, He R, Yu W, Li C, Cheng H, Zhu B, Yan J. ORAI3 contributes to hypoxia-inducible factor 1/2α-sensitive colon cell migration. Physiol Int. 2021 Jun 22. doi: 10.1556/2060.2021.00137. Epub ahead of print. PMID: 34161303. 2. Theriault JR, Felts AS, Bates BS, Perez JR, Palmer M, Gilbert SR, Dawson ES, Engers JL, Lindsley CW, Emmitte KA. Discovery of a new molecular probe ML228: an activator of the hypoxia inducible factor (HIF) pathway. Bioorg Med Chem Lett. 2012 Jan 1;22(1):76-81. doi: 10.1016/j.bmcl.2011.11.077. Epub 2011 Nov 28. PMID: 22172704; PMCID: PMC3251333. 3. Endo Y, Baldino K, Li B, Zhang Y, Sakthivel D, MacArthur M, Panayi AC, Kip P, Spencer DJ, Jasuja R, Bagchi D, Bhasin S, Nuutila K, Neppl RL, Wagers AJ, Sinha I. Loss of ARNT in skeletal muscle limits muscle regeneration in aging. FASEB J. 2020 Dec;34(12):16086-16104. doi: 10.1096/fj.202000761RR. Epub 2020 Oct 8. PMID: 33064329; PMCID: PMC7756517. 4. Chen H, Li J, Liang S, Lin B, Peng Q, Zhao P, Cui J, Rao Y. Effect of hypoxia-inducible factor-1/vascular endothelial growth factor signaling pathway on spinal cord injury in rats. Exp Ther Med. 2017 Mar;13(3):861-866. doi: 10.3892/etm.2017.4049. Epub 2017 Jan 16. PMID: 28450910; PMCID: PMC5403438.

In vitro protocol:

In vivo protocol:

1. Endo Y, Baldino K, Li B, Zhang Y, Sakthivel D, MacArthur M, Panayi AC, Kip P, Spencer DJ, Jasuja R, Bagchi D, Bhasin S, Nuutila K, Neppl RL, Wagers AJ, Sinha I. Loss of ARNT in skeletal muscle limits muscle regeneration in aging. FASEB J. 2020 Dec;34(12):16086-16104. doi: 10.1096/fj.202000761RR. Epub 2020 Oct 8. PMID: 33064329; PMCID: PMC7756517. 2. Chen H, Li J, Liang S, Lin B, Peng Q, Zhao P, Cui J, Rao Y. Effect of hypoxia-inducible factor-1/vascular endothelial growth factor signaling pathway on spinal cord injury in rats. Exp Ther Med. 2017 Mar;13(3):861-866. doi: 10.3892/etm.2017.4049. Epub 2017 Jan 16. PMID: 28450910; PMCID: PMC5403438.

1: Theriault JR, Perez J, Gilbert S, et al. Discovery of a Small Molecule Activator of the Hypoxia Inducible Factor Pathway. In: Probe Reports from the NIH Molecular Libraries Program. Bethesda (MD): National Center for Biotechnology Information (US); March 31, 2011. 2: Theriault JR, Felts AS, Bates BS, et al. Discovery of a new molecular probe ML228: an activator of the hypoxia inducible factor (HIF) pathway. Bioorg Med Chem Lett. 2012;22(1):76-81. doi:10.1016/j.bmcl.2011.11.077 3: Chen H, Li J, Liang S, et al. Effect of hypoxia-inducible factor-1/vascular endothelial growth factor signaling pathway on spinal cord injury in rats. Exp Ther Med. 2017;13(3):861-866. doi:10.3892/etm.2017.4049