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BACE1/2-IN-1 (化合物 34) 是有效的BACE1和BACE2抑制剂,IC50分别为 0.01 和 0.0053 μM。BACE1/2-IN-1 具有较低的 Pgp 外排比和改善的被动渗透率。BACE1/2-IN-1 在肝脏微粒体中代谢稳定性降低。
BACE1/2-IN-1 (化合物 34) 是有效的BACE1和BACE2抑制剂,IC50分别为 0.01 和 0.0053 μM。BACE1/2-IN-1 具有较低的 Pgp 外排比和改善的被动渗透率。BACE1/2-IN-1 在肝脏微粒体中代谢稳定性降低。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
25 mg | ¥ 10,600 | 6-8周 | |
50 mg | ¥ 13,800 | 6-8周 | |
100 mg | ¥ 17,500 | 6-8周 |
产品描述 | BACE1/2-IN-1 (compound 34) is an effective BACE1 and BACE2 inhibitor with IC50 of 0.01 and 0.0053 μM, respectively. BACE1/2-IN-1 has lower Pgp efflux ratio and improved passive permeability. The metabolic stability of BACE1/2-IN-1 in liver microsomes is decreased. |
体外活性 | BACE1/2-IN-1 (compound 34) demonstrates slight selectivity for BACE2 and retained >3000 fold selectivity against Cathepsin D [1]. |
体内活性 | 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]. |
分子量 | 401.57 |
分子式 | C21H31N5OS |
CAS No. | 2671036-34-1 |
存储 | Shipping with blue ice. |
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