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

DG051 

Cat. No.: HY-10825 Purity: 99.76%
Handling Instructions

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

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 540 In-stock
Estimated Time of Arrival: December 31
1 mg USD 144 In-stock
Estimated Time of Arrival: December 31
5 mg USD 576 In-stock
Estimated Time of Arrival: December 31
10 mg   Get quote  
50 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

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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].

Molecular Weight

426.33

Formula

C₂₁H₂₅Cl₂NO₄

CAS No.

929915-58-2

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 325 mg/mL (762.32 mM)

*"≥" 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
10 mM 0.2346 mL 1.1728 mL 2.3456 mL
*Please refer to the solubility information to select the appropriate solvent.
References

Purity: 99.76%

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Keywords:

DG051DG 051DG-051AminopeptidaseInhibitorinhibitorinhibit

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Product name:
DG051
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HY-10825
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