| Size | Price | Stock | Qty |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg | |||
| 250mg | |||
| 500mg | |||
| Other Sizes |
| Targets |
12/15-LOX (15-lipoxygenase-1).
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|---|---|
| ln Vitro |
As shown by caspase activity, ML351 (1-50 μM; 24 hours) had no negative effects on cell sterilization [2]. In a T1D model of liver cancer, ML351 (10-50 μM; 24 hours) protects islets against damage. Pro-inflammatory cytokine islets exhibited reduced insulin release in response to 25 mM and enhanced insulin release at 2.5 mM. However, ML351 significantly boosted insulin release in response to 25 mM compared to treatment with pro-inflammatory cytokines alone, and 2.5 mmol/L insulin returned insulin to amygdaloid island levels [2]. Insulin islets generated in vitro in response to pro-inflammatory cytokines are stimulated by ROS, whereas ML351 blocks this effect [2].
ML 351 is a potent and selective inhibitor of 15-LOX-1 with an IC50 of 200 nM. It exhibits >250-fold selectivity over related isozymes including 5-LOX, platelet 12-LOX, 15-LOX-2, ovine COX-1, and human COX-2. The compound is cell-permeable and exhibits protective effects against oxidative glutamate toxicity in mouse neuronal HT22 cells. ML 351 has nanomolar potency and excellent selectivity, making it a valuable tool for studying lipid metabolism in disease mechanisms. |
| ln Vivo |
In the STZ beta cell injury model, ML351 (0-48 mg/kg; administered before to the initiation of the STZ series and concluded five days following the final STZ dosage) inhibits the development of diabetes. In comparison to controls, there was a significant reduction in weight loss with 24 mg/kg (M24) + STZ ML351. M24 demonstrated nearly total protection against high blood pressure. However, by the ninth day of the trial, GTT was markedly obese and M48 and M0 showed significant hypertension [2]. The use of ML351 (intraperitoneal injection; 0–24 mg/kg; once daily for two weeks) improved hypertension and significantly decreased insulitis. It is believed that decreased β-cell mortality in NOD mice lessens insulitis, potentially by lowering the chemotactic signals that dead β-cells release. Animals with NOD+M24 had superior blood pressure management than those with NOD+M0 [2].
In vivo efficacy data for ML 351 is limited. The compound is primarily used as an in vitro tool for studying 12/15-LOX biology in inflammation, oxidative stress, and cancer. It exhibits protective effects against oxidative glutamate toxicity in neuronal cells, suggesting potential neuroprotective activity. Further in vivo studies would be needed to assess its therapeutic potential in inflammatory and neurodegenerative diseases. |
| Enzyme Assay |
The in vitro enzyme assay for 12/15-LOX inhibition uses recombinant human 15-LOX-1 enzyme and a fatty acid substrate (e.g., arachidonic acid or linoleic acid). The enzyme is incubated with the substrate and varying concentrations of ML 351 (typically 0.1 nM to 100 µM) at 25°C for 5-30 minutes. The reaction is stopped by acidification, and the product (hydroperoxy fatty acid) is extracted and analyzed by HPLC or by measuring absorbance at 234 nm. The IC50 is calculated from dose-response curves. Selectivity is determined by profiling against 5-LOX, platelet 12-LOX, 15-LOX-2, COX-1, and COX-2.
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| Cell Assay |
In vitro cellular assays are performed using mouse neuronal HT22 cells or other relevant cell lines. Cells are treated with ML 351 at concentrations ranging from 0.01 to 100 µM for 1-24 hours, then exposed to oxidative glutamate (5 mM) to induce toxicity. Cell viability is measured using MTT or Calcein-AM assays. Lipid peroxidation products (e.g., 4-HNE, MDA) are measured by ELISA or LC-MS. For cancer biology studies, cell proliferation and migration assays are performed in cancer cell lines treated with ML 351.
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| Animal Protocol |
Animal/Disease Models: Nineweeks old male C57BL/6J mice [2]
Doses: 0 mg/kg; 24 mg/kg; 48 mg/kg; Route of Administration: intraperitoneal (ip) injection before the start of the STZ series and after the last STZ dose Results after 5 days: Prevention of development of diabetes in STZ β-cell injury model that mimics T1D inflammation. Animal/Disease Models: Female NOD mice develop spontaneous autoimmune diabetes between 12 and 24 weeks of age [2] Doses: 0 mg/kg; 24 mg/kg; 48 mg/kg; Dosing: Before beginning the STZ series intraperitoneal (ip) injections were administered 5 days after the last STZ dose. Experimental Results: Prevention of early glycemic deterioration in NOD mice. In vivo animal model data for ML 351 is not extensively reported in the literature. As a research tool for studying 12/15-LOX biology in inflammation and oxidative stress, the compound would typically be evaluated in mouse models of neuroinflammation or oxidative stress-related diseases. Standard efficacy studies would involve compound administration (oral or intraperitoneal) followed by assessment of inflammatory markers, oxidative stress parameters, and tissue pathology. Pharmacokinetic studies would assess oral bioavailability, plasma half-life, and tissue distribution. |
| ADME/Pharmacokinetics |
ML 351 has a molecular weight of approximately 370 g/mol. The compound is cell-permeable and soluble in DMSO. It should be stored as a powder at -20°C. Pharmacokinetic parameters such as oral bioavailability, plasma half-life, and tissue distribution are not extensively characterized in publicly available literature. As a research compound, it is typically used in in vitro assays at concentrations ranging from nanomolar to low micromolar.
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| Toxicity/Toxicokinetics |
No detailed toxicity data is publicly available for ML 351. As a research compound, it is not intended for human use and has not undergone formal toxicological evaluation. Standard preclinical safety assessments for lipoxygenase inhibitors would typically include selectivity profiling against a panel of related enzymes to assess off-target effects, hERG channel inhibition for cardiac safety, and CYP450 enzyme inhibition for drug-drug interaction potential. The compound is supplied as a solid and should be stored desiccated at -20°C.
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| References | |
| Additional Infomation |
ML 351 is a research-grade 12/15-LOX inhibitor with >250-fold selectivity over related isozymes. It is not approved for clinical use. The compound exhibits protective effects against oxidative glutamate toxicity in neuronal cells, suggesting potential neuroprotective applications. ML 351 is widely applied in preclinical studies to clarify the role of lipid metabolism in disease mechanisms and to assess therapeutic potential in inflammatory disorders. It is supplied as a solid with high purity and should be stored desiccated at -20°C.
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| Molecular Formula |
C15H11N3O
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|---|---|
| Molecular Weight |
249.273
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| Exact Mass |
249.09
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| CAS # |
847163-28-4
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| PubChem CID |
664510
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| Appearance |
White to light yellow solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
507.3±60.0 °C at 760 mmHg
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| Flash Point |
260.6±32.9 °C
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| Vapour Pressure |
0.0±1.3 mmHg at 25°C
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| Index of Refraction |
1.672
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| LogP |
2.74
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
19
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| Complexity |
364
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
DYXYXTDIFMDJIR-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C15H11N3O/c1-17-15-13(9-16)18-14(19-15)12-8-4-6-10-5-2-3-7-11(10)12/h2-8,17H,1H3
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| Chemical Name |
5-(methylamino)-2-naphthalen-1-yl-1,3-oxazole-4-carbonitrile
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| Synonyms |
ML351 ML-351 ML 351
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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 |
| 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) |
DMSO : ~50 mg/mL (~200.59 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (8.34 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 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.0117 mL | 20.0586 mL | 40.1171 mL | |
| 5 mM | 0.8023 mL | 4.0117 mL | 8.0234 mL | |
| 10 mM | 0.4012 mL | 2.0059 mL | 4.0117 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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