BACE1/2-IN-1 

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].

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

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

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

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].

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

401.57

C₂₁H₃₁N₅OS

2671036-34-1

NC1=N[C@](CN(C2=NC=CC=N2)C3)([C@]4([H])C[C@]4(C(C)(C)OC[C@@H]5C[C@H]5C)[H])[C@@H]3CS1

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [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.  [Content Brief]