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

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

For research use only. We do not sell to patients.

DG051 Chemical Structure

DG051 Chemical Structure

CAS No. : 929915-58-2

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Solid + Solvent
10 mM * 1 mL in DMSO
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10 mM * 1 mL in DMSO USD 154 In-stock
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5 mg USD 140 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

Top Publications Citing Use of Products

1 Publications Citing Use of MCE DG051

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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]

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].

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

Molecular Weight

426.33

Formula

C21H25Cl2NO4

CAS No.
Appearance

Solid

Color

White to light yellow

SMILES

Cl[H].O=C(O)CCCN1CCC[C@H]1COC(C=C2)=CC=C2OC3=CC=C(Cl)C=C3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

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

Solvent & Solubility
In Vitro: 

DMSO : ≥ 325 mg/mL (762.32 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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  • Dilution Calculator

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.86%

References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 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
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DG051 Related Classifications

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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Product Name:
DG051
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HY-10825
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