Home>>Signaling Pathways>> Proteases>> Aminopeptidase>>DG-051
DG-051 Catalog No.GC18471

Size Price Stock Qty
1mg
$31.00
In stock
5mg
$140.00
In stock
10mg
$247.00
In stock
25mg
$542.00
In stock

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Sample solution is provided at 25 µL, 10mM.

Quality Control

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Chemical Properties

Cas No. 929915-58-2 SDF Download SDF
Synonyms N/A
Chemical Name (2S)-2-[[4-(4-chlorophenoxy)phenoxy]methyl]-1-pyrrolidinebutanoic acid, monohydrochloride
Canonical SMILES ClC1=CC=C(OC2=CC=C(OC[C@@H]3CCCN3CCCC(O)=O)C=C2)C=C1.Cl
Formula C21H24ClNO4.HCl M.Wt 426.3
Solubility Soluble in DMSO Storage Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
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Background

DG-051 is a potent, orally bioavailable leukotriene A4 hydrolase (LTA4H) inhibitor (Kd = 25 nM; IC50 = 47 nM), the enzyme that catalyzes the rate-determining step in the synthesis of LTB4 . However, it also inhibits the aminopeptidase activity of LTA4H with IC50 values of 72 and 150 nM when tested using the substrates L-alanine p-nitroanaline and prolyl-glycyl-proline peptide , respectively, potentially leading to PGP accumulation in vivo. DG-051 does not show any inhibitory activity against a panel of more than 50 additional aminopeptidases, ion channels, or HERG.

References:
[1].Sandanayaka, V., Mamat, B., Mishra, R.K., et al. Discovery of 4-[(2S)-2-{[4-(4-chlorophenoxy)phenoxy]methyl}-1-pyrrolidinyl]butanoic acid (DG-051) as a novel leukotriene A4 hydrolase inhibitor of leukotriene B4 biosynthesis J. Med. Chem. 53(2), 573-585 (2010).
[2]. Low, C.M., Akthar, S., Patel, D.F., et al. The development of novel LTA4H modulators to selectively target LTB4 generation Sci. Rep. 7, 44449 (2017).