| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
polyamine oxidase (PAO)[1]
The primary target of MDL 72527 is polyamine oxidase (PAO), a key enzyme in the polyamine catabolic pathway. It is a specific inhibitor of mammalian polyamine oxidase. By inhibiting PAO, it disrupts the oxidation of polyamines, which are essential cellular molecules involved in various biological processes. |
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| ln Vitro |
MDL 72527 dihydrochloride (300 µM; 24 h) significantly altered the morphology of M14 WT cells, resulting in the formation of several lysosomes and cytoplasmic vacuoles [2].
In vitro, MDL 72527 potently inhibits spermine oxidase and N1-acetylpolyamine oxidase with IC50 values of 6.1 µM and 0.02 µM, respectively. It is a selective inhibitor, showing no activity against monoamine oxidase or D-amino acid oxidase. |
| ln Vivo |
Neuroprotective properties of MDL 72527 dihydrochloride (100 mg/kg; ip; once) on neuronal cell death following transient localized cerebral ischemia[1].
In vivo, MDL 72527 has demonstrated neuroprotective effects and anticancer activity. It has been shown to exhibit a lysosomotropic effect. It is used as a research tool to study the role of polyamine metabolism in various physiological and pathological processes. |
| Enzyme Assay |
Non-cellular assays for MDL 72527 typically involve measuring its inhibitory activity against purified polyamine oxidase enzymes. The compound is incubated with the enzyme and its substrate, and the enzyme activity is measured using fluorometric or spectrophotometric methods. IC50 values are determined from dose-response curves.
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| Cell Assay |
Cell Cytotoxicity Assay[2]
Cell Types: M14 cells Tested Concentrations: 300 µM Incubation Duration: 24 h Experimental Results: demonstrated no significant effect on cell survival of melanoma cells. In vitro cellular assays for MDL 72527 are conducted using various cell lines to assess its effects on polyamine metabolism, cell proliferation, and survival. Cells are treated with the compound, and polyamine levels, cell viability, and markers of apoptosis are measured. These studies help elucidate the role of PAO in cellular processes. |
| Animal Protocol |
Animal/Disease Models: 250-300 g, Male spontaneously hypertensive rats (SHRs)[1]
Doses: 100 mg/kg Route of Administration: Ip; after the induction of ischemia Experimental Results: Dramatically decreased meanarterial blood pressure, changed the brain edema formation from 85.7 ± 0.3 to 84.5 ± 0.9% in cortex and from 79.9 ± 1.7 to 78.4 ± 2.0% in subcortex (difference not significant), decreased ischemic injury volume by 22% in the cortex and 17% in the subcortex. In vivo animal experiments for MDL 72527 are conducted in models of cancer, neurodegeneration, or other diseases where polyamine metabolism is implicated. The compound is administered via injection, and its effects on tumor growth, neurological function, or other disease endpoints are assessed. |
| ADME/Pharmacokinetics |
Pharmacokinetic properties of MDL 72527 are not extensively detailed. The compound has a molecular weight of 265.23 g/mol and a formula of C12H20N2·2HCl. It is soluble in DMSO and should be stored at -20°C. Its absorption, distribution, metabolism, and excretion have not been fully characterized.
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| Toxicity/Toxicokinetics |
Toxicological data for MDL 72527 are limited, as it is primarily a research reagent. It is for research use only and should not be administered to humans. Standard laboratory safety precautions should be followed when handling the compound.
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| References |
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| Additional Infomation |
Mdl-72527 is a dihydrochloride salt; the parent compound's RN is unavailable (6/85); a polyamine oxidase inhibitor.
MDL 72527 is a specific, small-molecule inhibitor of polyamine oxidase. It is also known as N1,N4-bis(2,3-butadienyl)-1,4-butanediamine dihydrochloride. It is a valuable tool for studying the role of polyamine catabolism in cellular physiology, cancer, and neurodegeneration. |
| Molecular Formula |
C12H22CL2N2
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|---|---|
| Molecular Weight |
265.22
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| Exact Mass |
264.116
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| CAS # |
93565-01-6
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| PubChem CID |
3035046
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| Appearance |
White to off-white solid powder
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| Boiling Point |
300.7ºC at 760mmHg
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| Flash Point |
159.2ºC
|
| Index of Refraction |
1.536
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| LogP |
4.013
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
9
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| Heavy Atom Count |
16
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| Complexity |
184
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| Defined Atom Stereocenter Count |
0
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| SMILES |
Cl.C(=CCNCCCCNCC=C=C)=C
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| InChi Key |
ITVRWVVFVHINOH-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C12H20N2.2ClH/c1-3-5-9-13-11-7-8-12-14-10-6-4-2;;/h5-6,13-14H,1-2,7-12H2;2*1H
|
| Chemical Name |
N,N'-bis(buta-2,3-dienyl)butane-1,4-diamine;dihydrochloride
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
H2O: 100 mg/mL (377.05 mM)
DMSO: 12.5 mg/mL (47.13 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.25 mg/mL (4.71 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 12.5 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 1.25 mg/mL (4.71 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 12.5 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. View More
Solubility in Formulation 3: 50 mg/mL (188.52 mM) in Saline (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.7705 mL | 18.8523 mL | 37.7045 mL | |
| 5 mM | 0.7541 mL | 3.7705 mL | 7.5409 mL | |
| 10 mM | 0.3770 mL | 1.8852 mL | 3.7705 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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