Lalistat 1

Names

[ Name ]:
Lalistat 1

Biological Activity

[Description]:

Lalistat 1 is a potent, selective, and competitive inhibitor of lysosomal acid lipase (LAL) and against purified human LAL (phLAL) with an IC50 of 68 nM. Lalistat 1 is a inhibitor of immunoglobulin A1 protease (IgA1P) proteases for H. influenzae, has less effects on other serine hydrolases (trypsin or β-lactamase, etc.). Lalistat 1 can be used for the research of niemann-pick type C (NPC) disease[2].

[Related Catalog]:

Research Areas >> Infection

Research Areas >> Neurological Disease

Signaling Pathways >> Anti-infection >> Bacterial

[Target]

IC50: 68 nM ( human LAL)[1]

[In Vitro]

Lalistat 1 (0-100 μM) shows activity against different non-typeable H. influenzae (NTHi) IgAP variants from clinical isolates in Elisa assay. It shows a dose-dependent inhibition of IgA1P B1 and B2, but at higher inhibitor concentrations, consistent with the higher expression levels of these variants. Nearly complete inhibition of IgA1P B1 and B2 is observed at 50 μM, with complete inhibition at 100 μM[1].

[References]

[1]. Anton I Rosenbaum , et al. Thiadiazole carbamates: potent inhibitors of lysosomal acid lipase and potential Niemann-Pick type C disease therapeutics. J Med Chem . 2010 Jul 22;53(14):5281-9.

[2]. Livia Shehaj, et al. Small-Molecule Inhibitors of Haemophilus influenzae IgA1 Protease.ACS Infect Dis. 2019 Jul 12;5(7):1129-1138.

Chemical & Physical Properties

[ Molecular Formula ]:
C₁₂H₁₈N₄O₃S

[ Molecular Weight ]:
298.36

Safety Information

[ Hazard Codes ]:
Xi

Related Compounds

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