ML351
Based on 4 publication(s) in Google Scholar
ML351 is a potent and highly specific 15-LOX-1 inhibitor with an IC50 of 200 nM. ML351 shows excellent selectivity (>250-fold) versus the related isozymes, 5-LOX, platelet 12-LOX, 15-LOX-2, ovine COX-1, and human COX-2. ML351 prevents dysglycemia and reduces β-cell oxidative stress in nonobese diabetic mouse model of T1D.
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- Purity : 99.16%
- CAS No.: 847163-28-4
- 화학식: C15H11N3O
- 분자량:249.27
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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용액&용해도
- Protocol
- 순도&문서
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) ML351
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Biological Activity
제품 설명
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Sf9 | IC50 |
0.12 μM
Compound: ML351
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Inhibition of human N-terminal His6-tagged 15-LOX-1 R402L mutant expressed in sf9 cells using arachidonic acid or linoleic acid as substrate by UV-Visible spectrophotometric analysis
Inhibition of human N-terminal His6-tagged 15-LOX-1 R402L mutant expressed in sf9 cells using arachidonic acid or linoleic acid as substrate by UV-Visible spectrophotometric analysis
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[PMID: 27647374] |
| Sf9 | IC50 |
0.18 μM
Compound: ML351
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Inhibition of human N-terminal His6-tagged 15-LOX-1 I417A mutant expressed in sf9 cells using arachidonic acid or linoleic acid as substrate by UV-Visible spectrophotometric analysis
Inhibition of human N-terminal His6-tagged 15-LOX-1 I417A mutant expressed in sf9 cells using arachidonic acid or linoleic acid as substrate by UV-Visible spectrophotometric analysis
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[PMID: 27647374] |
| Sf9 | IC50 |
0.26 μM
Compound: ML351
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Inhibition of human N-terminal His6-tagged 15-LOX-1 R404L mutant expressed in sf9 cells using arachidonic acid or linoleic acid as substrate by UV-Visible spectrophotometric analysis
Inhibition of human N-terminal His6-tagged 15-LOX-1 R404L mutant expressed in sf9 cells using arachidonic acid or linoleic acid as substrate by UV-Visible spectrophotometric analysis
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[PMID: 27647374] |
| Sf9 | IC50 |
0.3 μM
Compound: ML351
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Inhibition of human N-terminal His6-tagged 15-LOX-1 Q547L mutant expressed in sf9 cells using arachidonic acid as substrate by UV-Visible spectrophotometric analysis
Inhibition of human N-terminal His6-tagged 15-LOX-1 Q547L mutant expressed in sf9 cells using arachidonic acid as substrate by UV-Visible spectrophotometric analysis
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[PMID: 27647374] |
| Sf9 | IC50 |
0.33 μM
Compound: ML351
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Inhibition of wild type human N-terminal His6-tagged 15-LOX-1 expressed in sf9 cells using arachidonic acid or linoleic acid as substrate by UV-Visible spectrophotometric analysis
Inhibition of wild type human N-terminal His6-tagged 15-LOX-1 expressed in sf9 cells using arachidonic acid or linoleic acid as substrate by UV-Visible spectrophotometric analysis
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[PMID: 27647374] |
| Sf9 | IC50 |
0.39 μM
Compound: ML351
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Inhibition of human N-terminal His6-tagged 15-LOX-1 L407A mutant expressed in sf9 cells using arachidonic acid as substrate by UV-Visible spectrophotometric analysis
Inhibition of human N-terminal His6-tagged 15-LOX-1 L407A mutant expressed in sf9 cells using arachidonic acid as substrate by UV-Visible spectrophotometric analysis
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[PMID: 27647374] |
| Sf9 | IC50 |
0.77 μM
Compound: ML351
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Inhibition of human N-terminal His6-tagged 15-LOX-1 F414W mutant expressed in sf9 cells using arachidonic acid as substrate by UV-Visible spectrophotometric analysis
Inhibition of human N-terminal His6-tagged 15-LOX-1 F414W mutant expressed in sf9 cells using arachidonic acid as substrate by UV-Visible spectrophotometric analysis
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[PMID: 27647374] |
| Sf9 | IC50 |
0.87 μM
Compound: ML351
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Inhibition of human N-terminal His6-tagged 15-LOX-1 E356Q mutant expressed in sf9 cells using arachidonic acid as substrate by UV-Visible spectrophotometric analysis
Inhibition of human N-terminal His6-tagged 15-LOX-1 E356Q mutant expressed in sf9 cells using arachidonic acid as substrate by UV-Visible spectrophotometric analysis
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[PMID: 27647374] |
| Sf9 | IC50 |
4.1 μM
Compound: ML351
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Inhibition of human N-terminal His6-tagged 15-LOX-1 F414I mutant expressed in sf9 cells using arachidonic acid or linoleic acid as substrate by UV-Visible spectrophotometric analysis
Inhibition of human N-terminal His6-tagged 15-LOX-1 F414I mutant expressed in sf9 cells using arachidonic acid or linoleic acid as substrate by UV-Visible spectrophotometric analysis
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[PMID: 27647374] |
In Vitro
ML351 (1-50 μM; 24 hours) displays no deleterious effects on cellular apoptosis (by caspase activity assay)[2].ML351 (10-50 μM; 24 h) protects mouse islets in a T1D model in vitro. Islets exposed to proinflammatory cytokines exhibits increased insulin release at 2.5 mM glucose and impaired insulin release in response to 25 mM glucose. However, ML351 restores insulin secretion at 2.5 mmol/L glucose to control levels, and insulin release in response to 25 mM glucose is significantly improved compared with treatment with proinflammatory cytokines alone[2].ML351 reverses the stimulation of ROS production in mouse islets in response to proinflammatory cytokines in vitro[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Nine-week-old male C57BL/6J mice[2]
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Dosage:0 mg/kg; 24 mg/kg; 48 mg/kg;
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Administration:Intraperitoneal injection before the beginning of the STZ series and concluding 5 days after the last dose of STZ
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Result:Protected against diabetes development in an STZ β-cell injury model that mimics the inflammation seen in T1D.
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Animal Model:Female NOD mice develop spontaneous autoimmune diabetes between 12 and 24 weeks of age[2]
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Dosage:0 mg/kg; 24 mg/kg; 48 mg/kg;
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Administration:Intraperitoneal injection before the beginning of the STZ series and concluding 5 days after the last dose of STZ
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Result:Protected Against Early Glycemic Deterioration in NOD Mice.
Chemical Information
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CAS No. 847163-28-4
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Appearance Solid
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분자량 249.27
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화학식 C15H11N3O
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Color White to light yellow
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SMILES
N#CC1=C(NC)OC(C2=C3C=CC=CC3=CC=C2)=N1
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (4)
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Journal Impact Factor
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Most Recent
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J Nanobiotechnology
A therapeutic relay strategy enabled by spatiotemporally programmable nanoplatforms for multilayered cardioprotection against MI/RI. [Abstract]2026 May 27. PMID: 42204698 -
Phytomedicine
Molecular mechanisms of shenhong tongluo formula against myocardial ischemia-reperfusion injury: Insights from RNA sequencing, bioinformatics, reverse network pharmacology, molecular docking, and molecular dynamics simulations combined with experimental studies. [Abstract]2026 Jun:155:157896. PMID: 41921237 -
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bioRxiv
Chronic intermittent ethanol produces nociception through endocannabinoid-independent mechanisms in mice. [Abstract]2025 Feb 4:2024.11.08.622656. PMID: 39975399
용액&용해도
In Vitro:
DMSO : 50 mg/mL (200.59 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 0.5% CMC-Na/saline water
Solubility: 5 mg/mL (20.06 mM); Suspended solution; Need ultrasonic
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
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ROS/oxidative-stress fluorescent staining
ROS/oxidative-stress fluorescent staining uses cell-permeant fluorogenic probes that become fluorescent after oxidation inside cells or tissues; commonly used examples include DCFH-DA/DCFDA for broad cellular oxidant detection, DHE for superoxide-related signal detection, MitoSOX for mitochondrial superoxide-related signal detection, and CellROX probes for oxidative-stress-associated fluorescence readouts. The assay detects probe oxidation rather than a single ROS species unless the probe and analysis method have been chemically validated for that species. DCFH-DA enters cells, is deacetylated by intracellular esterases to DCFH, and produces fluorescent DCF after oxidation, so the readout is used as an operational measure of total cellular oxidative stress rather than a species-specific ROS measurement. DHE and MitoSOX can report superoxide-related oxidation, but red fluorescence alone can include non-specific ethidium-like oxidation products; HPLC or optimized spectral approaches are
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How to Choose the Right Model Animal
Choosing the right model animal is a validity-driven decision in which the species, strain, sex, age, genetic background, disease-induction method, outcome measures, and welfare burden must match the scientific question rather than laboratory tradition or convenience. A model should be selected by judging face validity, construct validity, and predictive validity: whether it resembles the human phenotype, whether it reproduces relevant mechanisms, and whether results are likely to predict human biology or treatment response. Animal studies often fail to translate because of species differences, weak disease resemblance, poor experimental design, inadequate reporting, publication bias, and underuse of randomization, blinding, and sample-size justification. Unresolved questions include how to rank competing models objectively, how much human-disease complexity must be reproduced for a given objective, and when non-animal systems such as organoids, ex vivo tissue, or computational models
순도&문서
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Data Sheet (282 KB)
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SDS (479 KB)
- English - EN (479 KB)
- Français - FR (479 KB)
- Deutsch - DE (479 KB)
- Norwegian - NO (479 KB)
- Español - ES (479 KB)
- Swedish - SV (479 KB)
- Italian - IT (479 KB)
- Korean - KR (479 KB)
- Portuguese - PT (479 KB)
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Handling Instructions (2659 KB)
References
[1]. Thomas Gaberel, et al. Impact of 12/15-Lipoxygenase on Brain Injury After Subarachnoid Hemorrhage. Stroke. 2019 Feb;50(2):520-523. [Content Brief]
[2]. Ganesha Rai, et al. Discovery of ML351, a Potent and Selective Inhibitor of Human 15-Lipoxygenase-1 [Content Brief]
[3]. Marimar Hernandez-Perez, et al. Inhibition of 12/15-Lipoxygenase Protects Against β-Cell Oxidative Stress and Glycemic Deterioration in Mouse Models of Type 1 Diabetes. Diabetes. 2017 Nov;66(11):2875-2887. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 4.0117 mL | 20.0586 mL | 40.1171 mL | 100.2929 mL |
| 5 mM | 0.8023 mL | 4.0117 mL | 8.0234 mL | 20.0586 mL | |
| 10 mM | 0.4012 mL | 2.0059 mL | 4.0117 mL | 10.0293 mL | |
| 15 mM | 0.2674 mL | 1.3372 mL | 2.6745 mL | 6.6862 mL | |
| 20 mM | 0.2006 mL | 1.0029 mL | 2.0059 mL | 5.0146 mL | |
| 25 mM | 0.1605 mL | 0.8023 mL | 1.6047 mL | 4.0117 mL | |
| 30 mM | 0.1337 mL | 0.6686 mL | 1.3372 mL | 3.3431 mL | |
| 40 mM | 0.1003 mL | 0.5015 mL | 1.0029 mL | 2.5073 mL | |
| 50 mM | 0.0802 mL | 0.4012 mL | 0.8023 mL | 2.0059 mL | |
| 60 mM | 0.0669 mL | 0.3343 mL | 0.6686 mL | 1.6715 mL | |
| 80 mM | 0.0501 mL | 0.2507 mL | 0.5015 mL | 1.2537 mL | |
| 100 mM | 0.0401 mL | 0.2006 mL | 0.4012 mL | 1.0029 mL |
ML351 Related Classifications
HY-111310 Related Classifications
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