ML351 - CAS:847163-28-4

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ML351

目录号 : KM8445 CAS No. : 847163-28-4 纯度 : 98%

Data Sheet 产品使用指南

ML351 是一种有效且高度特异的 15-LOX-1 抑制剂，其 IC₅₀ of 200 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。

规格	价格	是否有货
5mg		In-stock
10mg		In-stock
25mg		In-stock
50mg		In-stock
100mg	询价	In-stock

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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.

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.

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.

分子式

C₁₅H₁₁N₃O

分子量

249.27

CAS号

847163-28-4

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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

溶解性数据

In Vitro:

DMSO : 50 mg/mL (200.59 mM; ultrasonic and warming and heat to 60°C)

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： 0.5% CMC-Na/saline water

Solubility: 5 mg/mL (20.06 mM); Suspended solution; Need ultrasonic

2.

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。

纯度： 98%

Data Sheet

产品使用指南

暂无相关参考文献

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量

浓度

体积

分子量*

重置计算

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2

浓度

体积

浓度

体积

重置计算

动物实验计算换算器

第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）

给药剂量

mg/kg

动物平均体重

每只动物给药体积

动物数量

只

第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系客服为您提供正确的澄清溶液配方）

% DMSO

% Tween 80

% ddH₂O

% DMSO

计算重置

计算结果:

工作液浓度： mg/ml；

DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系客服）；

体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL ddH₂O，混匀澄清。

配置后的溶液总体积：

注意：1. 首先保证母液是澄清的；
2. 一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。

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The molarity calculator equation

The dilution calculator equation

动物实验计算换算器