BACE1/2-IN-1

Names

[ CAS No. ]:
2671036-34-1

[ Name ]:
BACE1/2-IN-1

Biological Activity

[Description]:

BACE1/2-IN-1 (compound 34) is a potent BACE1 and BACE2 inhibitor, with an IC50 of 0.01 and 0.0053 μM, respectively. BACE1/2-IN-1 shows a combination of lower Pgp efflux ratio and improved passive permeability. BACE1/2-IN-1 displays reduced liver microsomal metabolic stability[1].

[Related Catalog]:

Signaling Pathways >> Neuronal Signaling >> Beta-secretase
Research Areas >> Neurological Disease

[Target]

IC50: 0.0053 μM (BACE2), 0.01 μM (BACE1), 160 μM (Cathepsin D)[1]


[In Vitro]

BACE1/2-IN-1 (compound 34) demonstrates slight selectivity for BACE2 and retained >3000 fold selectivity against Cathepsin D[1].

[In Vivo]

BACE1/2-IN-1 (compound 34) (PDAPP (V717F) transgenic mice, 0-100 mg/kg, Subcutaneous injection, once) shows significant reduction in PDAPP mouse cortex Aβ at 100 mg/kg (40%), and 30 mg/kg (24%), but not at 10 mg/kg (12%NS)[1].

[References]

[1]. Winneroski LL, et al. Preparation and biological evaluation of BACE1 inhibitors: Leveraging trans-cyclopropyl moieties as ligand efficient conformational constraints. Bioorg Med Chem. 2020 Jan 1;28(1):115194.

Chemical & Physical Properties

[ Molecular Formula ]:
C21H31N5OS

[ Molecular Weight ]:
401.57

Related Compounds