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DG-051
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
DG-051图片
CAS NO:929915-58-2
包装与价格：
包装价格(元)
1mg电议
5mg电议
10mg电议
25mg电议

产品介绍
DG-051 是一种有效的白三烯 A4 水解酶抑制剂，在酶试验中抑制白三烯 B4 的生物合成，IC50\u003d47 nM。
Cas No.929915-58-2
化学名(2S)-2-[[4-(4-chlorophenoxy)phenoxy]methyl]-1-pyrrolidinebutanoic acid, monohydrochloride
Canonical SMILESClC1=CC=C(OC2=CC=C(OC[C@@H]3CCCN3CCCC(O)=O)C=C2)C=C1.Cl
分子式C21H24ClNO4.HCl
分子量426.3
溶解度DMF: 20 mg/ml,DMSO: 12.5 mg/ml,Ethanol: 12.5 mg/ml,PBS (pH 7.2): 2 mg/ml
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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).