ML351|cas:847163-28-4|西域试剂

ML351,98.19%

产品编号：Bellancom-111310| CAS NO：847163-28-4| 分子式：C₁₅H₁₁N₃O| 分子量：249.27

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货号	价格	库存与货期
Bellancom-111310	￥1500.00	杭州北京（现货）
Bellancom-111310	￥2500.00	杭州北京（现货）
Bellancom-111310	￥5500.00	杭州北京（现货）
Bellancom-111310	￥9500.00	杭州北京（现货）
Bellancom-111310	￥0.00	杭州北京（现货）

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ML351

产品介绍

ML351 是一种有效且高度特异的 15-LOX-1 抑制剂，其 IC₅₀ of200 nM。ML351 对相关同工酶 (5-LOX、血小板 12-LOX、15-LOX-2、绵羊 COX-1 和人COX-2) 表现出良好的选择性(>250倍)。ML351 对 T1D 非肥胖糖尿病小鼠模型的血糖异常和β细胞氧化应激有抑制作用。

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.

体外研究

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 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.
ML351 reverses the stimulation of ROS production in mouse islets in response to proinflammatory cytokines in vitro.

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

体内研究

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.

西域 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.

体内研究

西域 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.

性状

Solid

溶解性数据

In Vitro:

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

配制储备液

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

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，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，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 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.

请依序添加每种溶剂： 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。