2. Neuronal Signaling
  3. Beta-secretase Amyloid-β
  4. BACE1/2-IN-1

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。

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BACE1/2-IN-1 Chemical Structure

BACE1/2-IN-1 Chemical Structure

CAS No. : 2671036-34-1

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BACE1/2-IN-1 相关抗体

Top Publications Citing Use of Products

查看 Beta-secretase 亚型特异性产品:

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BACE1 BACE2

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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 & Target

IC50: 0.0053 μM (BACE2), 0.01 μM (BACE1), 160 μM (Cathepsin D)[1]
细胞效力
(Cellular Effect)
Cell Line Type Value Description References
HEK293 IC50
0.01 μM
Compound: 34
Inhibition of human BACE1 (1 to 460 residues) expressed in HEK293 cells using mcaFRET peptide as substrate after 20 hrs by FRET assay
Inhibition of human BACE1 (1 to 460 residues) expressed in HEK293 cells using mcaFRET peptide as substrate after 20 hrs by FRET assay
[PMID: 31786008]
体外研究
(In Vitro)

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

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

BACE1/2-IN-1 相关抗体:
体内研究
(In Vivo)

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

401.57

Formula

C21H31N5OS
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

BACE1/2-IN-1 相关分类

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  • 稀释计算器

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

BACE1/2-IN-12671036-34-1Beta-secretaseAmyloid-βBACEβ-Secretase β-amyloid peptideAβAbetaMDCK cellsAlzheimer’s diseaseCyclopropylConformational constraintPDAPPInhibitorinhibitorinhibit

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