BACE1-IN-5 

BACE1-IN-5 (Compound 15) is a β-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitor with an IC₅₀ of 9.1 nM, and also inhibits cellular amyloid-β (Aβ) with an IC₅₀ of 0.82 nM. BACE1-IN-5 has a medicinal chemistry that improves hERG inhibition and P-gp efflux^[1].

BACE1-IN-5 (Compound 15; 1-3 mg/kg; oral administration; 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 demonstrats 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) ^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

461.41

C₁₈H₁₆F₅N₅O₂S

2581114-83-0

O=C(C1=NC=C(OCF)N=C1)NC2=CC=C(F)C([C@@]3(C)N=C(N)S[C@H](C(F)(F)F)C3)=C2

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• [1]. Kusakabe KI, et al. Trifluoromethyl Dihydrothiazine-Based β-Secretase (BACE1) Inhibitors with Robust Central Aβ Reduction and Minimal Covalent Binding Burden. ChemMedChem. 2019 Oct 27.  [Content Brief]