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ML351

人网织红细胞15-LO-1抑制剂，ML 351 is a selective 12/15 LOX inhibitor that is active in vivo.

目录号: PC11600 纯度: ≥98%

CAS No. :847163-28-4

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中文名称

ML351

英文名称

ML351

英文别名

ML351 NEW;Capecitabine-d11;ML 351;5-(Methylamino)-2-(1-naphthalenyl)-4-oxazolecarbonitrile;CID 664510;SID 104223766

Cas No.

847163-28-4

分子式

C₁₅H₁₁N₃O

分子量

249.27

包装储存

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

生物活性

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.

性状

Solid

体外研究(In Vitro)

ML351 (1-50 μM; 24 hours) displays no deleterious effects on cellular apoptosis (by caspase activity assay).
ML351 (10-50 μM; 24 h) protects mouse islets in a T1D model 体外研究. 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.
ML351 reverses the stimulation of ROS production in mouse islets in response to proinflammatory cytokines 体外研究.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

ML351 (0-48 mg/kg; before the beginning of the STZ series and concluding 5 days after the last dose of STZ) protects against diabetes development in an STZ β-cell injury model. ML351 at 24 mg/kg (M24)+ STZ shows significantly less weight reduction compares with control group. M24 shows almost complete protection from hyperglycemia. But M48 and M0 exhibits frank hyperglycemia by day 9 of the study and significantly impaired GTTs.
ML351 (intraperitoneal injection; 0-24 mg/kg; daily for 2 weeks) leads to improved glycemic control and significantly reduced insulitis. The reduction of β-cell death in NOD mice has been suggested to lead to reductions in insulitis, likely by mitigating the chemotactic signals released by dying β-cells. NOD + M24 animals exhibited improved glycemic control compared with NOD + M0 animals.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Nine-week-old male C57BL/6J mice
Dosage:	0 mg/kg; 24 mg/kg; 48 mg/kg;
Administration:	Intraperitoneal injection before the beginning of the STZ series and concluding 5 days after the last dose of STZ
Result:	Protected against diabetes development in an STZ β-cell injury model that mimics the inflammation seen in T1D.

Animal Model:	Female NOD mice develop spontaneous autoimmune diabetes between 12 and 24 weeks of age
Dosage:	0 mg/kg; 24 mg/kg; 48 mg/kg;
Administration:	Intraperitoneal injection before the beginning of the STZ series and concluding 5 days after the last dose of STZ
Result:	Protected Against Early Glycemic Deterioration in NOD Mice.

运输条件

Room temperature or refrigerated transportation.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

参考文献

[1]. Thomas Gaberel, et al. Impact of 12/15-Lipoxygenase on Brain Injury After Subarachnoid Hemorrhage. Stroke. 2019 Feb;50(2):520-523. [Information]

[2]. Ganesha Rai, et al. Discovery of ML351, a Potent and Selective Inhibitor of Human 15-Lipoxygenase-1 [Information]

[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. [Information]

溶解度数据

体外研究:

DMSO : 125 mg/mL (501.46 mM; Need ultrasonic)

配制储备溶液

浓度溶剂体积质量	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

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

建议依照次序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.08 mg/mL (8.34 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (8.34 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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