ML351 (Synonyms: CID 664510) |
| Catalog No.GC13386 |
ML351 is a selective 15-lipoxygenase-1 (15-LOX-1; 12/15-LOX) inhibitor with an IC50 of 200nM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 847163-28-4
Sample solution is provided at 25 µL, 10mM.
;)
_1-7.$$$37316672@70.jpg');)
;)
;)
_273-287.$$$36806353@46.jpg');)
_1-16.$$$37156877@44.jpg');)
;)
;)
;)
_1124-1138.$$$35908550@30.jpg');)
_766-780.$$$37100057@30.jpg');)
_418-432.$$$36893736@30.jpg');)
_240-255.$$$35108512@29.jpg');)
_533-545.$$$36543525@28.jpg');)
_264-276.$$$36600053@22.jpg');)
_2214998.$$$@0.jpg');)
ML351 is a selective 15-lipoxygenase-1 (15-LOX-1; 12/15-LOX) inhibitor with an IC50 of 200nM[1]. 15-LOX-1 is a member of the lipid oxidase family that can trigger phospholipid peroxidation in the plasma membrane. By inhibiting 15-LOX-1, ML351 can reduce the production of harmful oxidative products in cells[2].
In vitro, HT-22 cells treated with ML351 (0-10μM) dose-dependently reversed glutamate-induced cell death[1]. ML351 (10μM) treatment of peritoneal macrophages (PMφ) cells for 2 h inhibited the inflammatory response induced by Kdo2-Lipid A and suppressed the mRNA expression of 12/15LOX and inducible nitric oxide synthase (iNOS )[3].
In vivo, ML351 (50 mg/kg) treated with acute heart failure mice by subcutaneous injection significantly reduced myocardial infarction size on days 1 and 5, increased CD11b expression, and reduced inflammatory responses in the heart and spleen [3]. ML351 (24 mg/kg) treated with intraperitoneal injection in non-obese diabetic (NOD) mice for 8 weeks reduced blood glucose levels, reduced oxidative stress markers in pancreatic β cells, and increased antioxidant enzyme levels [4]. ML351 (50μM/kg) treated with intraperitoneal injection in rats undergoing orthodontic treatment for 14 days strongly inhibited orthodontic-induced root resorption (OIRR) and suppressed the appearance of osteoclasts and odontoclasts [5].
References:
[1] Rai G, Joshi N, Perry S, et al. Discovery of ML351, a potent and selective inhibitor of human 15-lipoxygenase-1[J]. Probe Reports from the NIH Molecular Libraries Program [Internet], 2014.
[2] Cakir-Aktas C, Bodur E, Yemisci M, et al. 12/15 Lipoxygenase Inhibition Attenuates Neuroinflammation by Suppressing Inflammasomes[J]. Frontiers in cellular neuroscience, 2023, 17: 1277268.
[3] Tourki B, Black L M, Kain V, et al. Lipoxygenase inhibitor ML351 dysregulated an innate inflammatory response leading to impaired cardiac repair in acute heart failure[J]. Biomedicine & Pharmacotherapy, 2021, 139: 111574.
[4] Hernandez-Perez M, Chopra G, Fine J, et al. Inhibition of 12/15-lipoxygenase protects against β-cell oxidative stress and glycemic deterioration in mouse models of type 1 diabetes[J]. Diabetes, 2017, 66(11): 2875-2887.
[5] Nashiro-Oyakawa Y, Hotokezaka Y, Hotokezaka H, et al. Inhibition of 12/15-lipoxygenase reduces orthodontically induced root resorption in rats[J]. The Angle Orthodontist, 2024.
|
Cell experiment [1]: |
|
|
Cell lines |
Peritoneal macrophage (PMϕ) |
|
Preparation method |
PMϕ were isolated from male C57BL/6 mice after injection of cold media (DMEM with 10% heat inactivated FBS, 1% antibiotic/antimycotic) into the peritoneal cavity. After 4–6 h at 37°C, 5% CO2 in the incubator, cells are well attached and ready for experiments. ML351 (10μM) was added in direct contact to the cells for 2 h. |
|
Reaction Conditions |
10 μM ; 2 h |
|
Applications |
ML351 decreased 12LOX gene expression (0.52 fold) and 15LOX gene expression (0.73 fold) with no change in 5LOX expression compared with the control group. |
|
Animal experiment [2]: |
|
|
Animal models |
NOD/ShiLTJ (NOD) mice |
|
Preparation method |
Six-week-old NOD mice were injected intraperitoneally with vehicle or 24 mg/kg ML351 daily for 2 weeks. |
|
Dosage form |
24 mg/kg; i.p. |
|
Applications |
Treatment of NOD mice with ML351 led to improved glycemic control and significantly reduced insulitis. |
|
References: |
|
| Cas No. | 847163-28-4 | SDF | |
| Synonyms | CID 664510 | ||
| Chemical Name | 5-(methylamino)-2-(1-naphthalenyl)-4-oxazolecarbonitrile | ||
| Canonical SMILES | CNC1=C(C#N)N=C(O1)C2=C3C(C=CC=C3)=CC=C2 | ||
| Formula | C15H11N3O | M.Wt | 249.3 |
| Solubility | ≤25mg/ml in DMSO; 25mg/ml in dimethyl formamide | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 4.0112 mL | 20.0562 mL | 40.1123 mL |
| 5 mM | 0.8022 mL | 4.0112 mL | 8.0225 mL |
| 10 mM | 0.4011 mL | 2.0056 mL | 4.0112 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 14 reference(s) in Google Scholar.)
GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
Required fields are marked with *