BACE1-IN-2

Names

[ Name ]:
BACE1-IN-2

[Synonym ]:
2-Pyridinecarboxamide, N-[3-[(2R,3R)-5-amino-3,6-dihydro-3-methyl-2-(trifluoromethyl)-2H-1,4-oxazin-3-yl]-4-fluorophenyl]-5-cyano-
N-{3-[(2R,3R)-5-Amino-3-methyl-2-(trifluoromethyl)-3,6-dihydro-2H-1,4-oxazin-3-yl]-4-fluorophenyl}-5-cyano-2-pyridinecarboxamide

Biological Activity

[Description]:

BACE1-IN-2 is a 1,4-Oxazine β-Secretase 1 (BACE1) inhibitor with an IC50 of 22 nM[1].

[Related Catalog]:

Signaling Pathways >> Neuronal Signaling >> Beta-secretase

Research Areas >> Neurological Disease

[Target]

IC50: 22 nM (BACE1)[1]

[In Vitro]

BACE1-IN-2 (Compound 3) is 10-fold more potent toward BACE1 than BACE2, inhibition of which may lead to hair depigmentation. BACE1-IN-2 inhibits hAβ42 cell with an IC50 of 6.0 nM[1].

[References]

[1]. Gijsen HJM, et al. Optimization of 1,4-Oxazine β-Secretase 1 (BACE1) Inhibitors Toward a Clinical Candidate. J Med Chem. 2018 Jun 28;61(12):5292-5303.

Chemical & Physical Properties

[ Density]:
1.5±0.1 g/cm3

[ Molecular Formula ]:
C₁₉H₁₅F₄N₅O₂

[ Molecular Weight ]:
421.35

[ Exact Mass ]:
421.116180

[ LogP ]:
1.61

[ Index of Refraction ]:
1.603

Related Compounds

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