BACE1-IN-5 is a BACE1 inhibitor (IC50: 9.1 nM) and also inhibits cellular amyloid-β (Aβ; IC50: 0.82 nM). BACE1-IN-5 has medicinal chemistry that improves hERG inhibition and P-gp efflux.

BACE1-IN-5 (Compound 15; 1-3 mg/kg; p.o.; for 2-6 hours; male ICR mice) treatment results in a significant and dose-dependent decrease of total Aβ, reduces total Aβ by 76% (4 hours) at a free brain concentration of 4.1 ng/mL (8.9 nM) at 1 mg/kg. BACE1-IN-5 demonstrates a K(p,uu) value of 1.3 at 1 mg/kg (4 hours time point). At 3 mg/kg, a maximum Aβ reduction of 87% is achieved at a free brain concentration of 9.5 ng/mL (21 nM).

T10453

C18H16F5N5O2S

461.41

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years