Acebilustat

Names

[ Name ]:
Acebilustat

[Synonym ]:
Benzoic acid, 4-[[(1S,4S)-5-[[4-[4-(2-oxazolyl)phenoxy]phenyl]methyl]-2,5-diazabicyclo[2.2.1]hept-2-yl]methyl]-
4-{[(1S,4S)-5-{4-[4-(1,3-Oxazol-2-yl)phenoxy]benzyl}-2,5-diazabicyclo[2.2.1]hept-2-yl]methyl}benzoic acid
acebilustat

Biological Activity

[Description]:

Acebilustat is a leukotriene A4 hydrolase inhibitor, used for an oral antiinflammatory drug.

[Related Catalog]:

Signaling Pathways >> Others >> Others

Research Areas >> Inflammation/Immunology

[In Vitro]

Acebilustat is a leukotriene A4 hydrolase inhibitor, which is safe and well tolerated in phase 1 trial[1]. Acebilustat is an antiinflammatory drug in development for the treatment of CF and other diseases. It is a potent inhibitor of the enzyme leukotriene A4 hydrolase (LTA4H), which catalyzes the rate-limiting step in the formation of leukotriene B4 (LTB4), a potent chemoattractant and activator of inflammatory immune cells including neutrophils[2].

[References]

[1]. Elborn JS, et al. Phase 1 Studies of Acebilustat: Biomarker Response and Safety in Patients with Cystic Fibrosis. Clin Transl Sci. 2016 Nov 2

[2]. Elborn JS, et al. Phase I Studies of Acebilustat: Pharmacokinetics, Pharmacodynamics, Food Effect, and CYP3A Induction. Clin Transl Sci. 2016 Oct 28.

[Related Small Molecules]

Chemical & Physical Properties

[ Density]:
1.3±0.1 g/cm3

[ Boiling Point ]:
649.1±65.0 °C at 760 mmHg

[ Molecular Formula ]:
C₂₉H₂₇N₃O₄

[ Molecular Weight ]:
481.542

[ Flash Point ]:
346.3±34.3 °C

[ Exact Mass ]:
481.200165

[ LogP ]:
4.37

[ Vapour Pressure ]:
0.0±2.0 mmHg at 25°C

[ Index of Refraction ]:
1.654

[ Storage condition ]:
2-8℃