BACE1/2-IN-1 (化合物 34) 是一种有效的BACE1和BACE2抑制剂，其IC50分别为 0.01 和 0.0053 μM。BACE1/2-IN-1 显示了较低的 Pgp 外排比和提高的被动渗透率。BACE1/2-IN-1 显示肝脏微粒体代谢稳定性降低。

BACE1/2-IN-1 (compound 34) is a potent BACE1 and BACE2 inhibitor, with an IC 50 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].

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

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].

2671036-34-1

C21H31N5OS

401.57

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