| Description | DG051 is a potent leukotriene A4 hydrolase (LTA4H) inhibitor (IC50: 47 nM). |
| In vitro | DG051是一种高效的LTA4H氨肽酶活性抑制剂，针对L-丙氨酸对硝基苯甲酰胺(IC50: 72 nM)。该化合物在人类全血(HWB)中的抑制作用IC50值为37 nM [1]。DG051为LTA4H抑制剂，目前正处于第二阶段临床开发阶段，用于预防心脏攻击[2]。 |
| Target activity | LTA4H:47 nM (IC50) |
| molecular weight | 426.33 |
| Molecular formula | C21H25Cl2NO4 |
| CAS | 929915-58-2 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 317 mg/mL (743.56 mM) |
| References | 1. Sandanayaka V, 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. 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. |