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

DG051 

目录号: HY-10825 纯度: 99.76%
产品使用指南

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
10 mM * 1 mL in DMSO ¥4502
In-stock
1 mg ¥1200
In-stock
5 mg ¥4800
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50 mg   询价  

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  • 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
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 : ≥ 325 mg/mL (762.32 mM)

* "≥" 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
10 mM 0.2346 mL 1.1728 mL 2.3456 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 (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。

参考文献

纯度: 99.76%

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

质量   浓度   体积   分子量 *
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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2

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产品名称:
DG051
目录号:
HY-10825
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