| Size | Price | Stock | Qty |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| Other Sizes |
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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].
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| 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].
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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. |
| References |
[1]. Thomas Gaberel, et al. Impact of 12/15-Lipoxygenase on Brain Injury After Subarachnoid Hemorrhage. Stroke. 2019 Feb;50(2):520-523.
[2]. Ganesha Rai, et al. Discovery of ML351, a Potent and Selective Inhibitor of Human 15-Lipoxygenase-1 [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. |
| Molecular Formula |
C15H11N3O
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|---|---|
| Molecular Weight |
249.273
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| Exact Mass |
249.0902
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| CAS # |
847163-28-4
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| SMILES |
N#CC1N=C(C2=CC=CC3=CC=CC=C23)OC=1NC
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| Synonyms |
ML351 ML-351 ML 351
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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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