1. Metabolic Enzyme/Protease
  2. Aminopeptidase
  3. DG051

DG051 是一种有效的白三烯 A4 水解酶 (leukotriene A4 hydrolase) 抑制剂,IC50 为 47 nM。

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DG051 Chemical Structure

DG051 Chemical Structure

CAS No. : 929915-58-2

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规格 价格 是否有货 数量
Free Sample (0.1 - 0.2 mg)   Apply now  
10 mM * 1 mL in DMSO ¥1540
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5 mg ¥1400
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10 mg ¥2400
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25 mg ¥5100
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50 mg ¥8100
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MCE 顾客使用本产品发表的 1 篇科研文献

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

DG051 is a potent leukotriene A4 hydrolase inhibitor of leukotriene B4 biosynthesis in the enzyme assay with an IC50=47 nM.

IC50 & Target

IC50: 47 nM (LTA4H)[1]

体外研究
(In Vitro)

DG051 is a potent inhibitor of LTA4H aminopeptidase activity against L-alanine p-nitroanilide (IC50=72 nM). DG051 inhibits human whole blood (HWB) with IC50 of 37 nM. As applied within the context of LTA4H inhibitor design, the chemistry team is able to design a potent DG051(Kd=26 nM) with high aqueous solubility (>30 mg/mL) and high oral bioavailability (>80% across species) that is currently undergoing clinical evaluation for the treatment of myocardial infarction and stroke[1] DG-051 is a first-in-class small molecule inhibitor of leukotriene A4 hydrolase (LTA4H), currently in Phase II clinical development for the prevention of heart attack[2].

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

分子量

426.33

Formula

C21H25Cl2NO4

CAS 号
性状

固体

颜色

White to light yellow

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
In Vitro: 

DMSO 中的溶解度 : ≥ 325 mg/mL (762.32 mM; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

* "≥" means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.3456 mL 11.7280 mL 23.4560 mL
5 mM 0.4691 mL 2.3456 mL 4.6912 mL
查看完整储备液配制表

* 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 (sealed storage, away from moisture)。-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。

  • 摩尔计算器

  • 稀释计算器

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

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料

纯度: 99.86%

参考文献

完整储备液配制表

* 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 (sealed storage, away from moisture)。-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。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.3456 mL 11.7280 mL 23.4560 mL 58.6400 mL
5 mM 0.4691 mL 2.3456 mL 4.6912 mL 11.7280 mL
10 mM 0.2346 mL 1.1728 mL 2.3456 mL 5.8640 mL
15 mM 0.1564 mL 0.7819 mL 1.5637 mL 3.9093 mL
20 mM 0.1173 mL 0.5864 mL 1.1728 mL 2.9320 mL
25 mM 0.0938 mL 0.4691 mL 0.9382 mL 2.3456 mL
30 mM 0.0782 mL 0.3909 mL 0.7819 mL 1.9547 mL
40 mM 0.0586 mL 0.2932 mL 0.5864 mL 1.4660 mL
50 mM 0.0469 mL 0.2346 mL 0.4691 mL 1.1728 mL
60 mM 0.0391 mL 0.1955 mL 0.3909 mL 0.9773 mL
80 mM 0.0293 mL 0.1466 mL 0.2932 mL 0.7330 mL
100 mM 0.0235 mL 0.1173 mL 0.2346 mL 0.5864 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Inquiry Information

产品名称:
DG051
目录号:
HY-10825
需求量: