DG051 - Aminopeptidase 抑制劑 - 生命科學試劑 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEDG051Cat. No.: HY-10825CAS No.: 929915-58-2分式: CHClNO分量: 426.33作靶點: Aminopeptidase作通路: Metabolic Enzyme/Protease儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實驗 DMSO : 325 mg/mL (762.32 mM)* means

2、soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 2.3456 mL 11.7280 mL 23.4560 mL5 mM 0.4691 mL 2.3456 mL 4.6912 mL10 mM 0.2346 mL 1.1728 mL 2.3456 mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存式和期限。BIOLOGICAL ACTIVITY物活性 DG051種有效的三烯 A4 解酶 (leukotriene A4 hydrolase) 抑制劑，I

3、C50 為 47 nM。IC50 & Target IC50: 47 nM (LTA4H) 1體外研究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 LTA4H1/2 Master of Small Molecules 您邊的抑制劑師www.MedC

4、hemEinhibitor 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 clinicalevaluation for the treatment of myocardial infarction and stroke 1 DG-051 is a first-in-c

5、lass small moleculeinhibitor of leukotriene A4 hydrolase (LTA4H), currently in Phase II clinical development for the prevention ofheart attack 2.REFERENCES1. Sandanayaka V, et al. Discovery of 4-(2S)-2-4-(4-chlorophenoxy)phenoxymethyl-1-pyrrolidinylbutanoic acid (DG-051) as a novelleukotriene A4 hyd

6、rolase inhibitor of leukotriene B4 biosynthesis. J Med Chem. 2010 Jan 28;53(2):573-85.2. Enache LA, et al. Synthesis and structural assignment of two major metabolites of the LTA4H inhibitor DG-051. Bioorg Med Chem Lett.2009 Nov 15;19(22):6275-9.McePdfHeightCaution: Product has not been fully validated for medical applications.For research use only.Tel: 400-8