| S2156 |
LY2886721
|
LY2886721是BACE抑制剂，用于治疗阿尔茨海默症。Phase 1/2。 |
-
Acta Neuropathol, 2025, 149(1):10
-
Foods, 2024, 13(18)2858
-
Stem Cell Reports, 2023, 18(7):1516-1533
|
|
| S1528 |
LY2811376
|
LY2811376是第一个口服有效的，非肽类β-secretase(BACE1)抑制剂，IC50为239 nM-249 nM，可以减少Aβ分泌，EC50为300 nM，作用于BACE1比作用于BACE2选择性高10倍，比作用于其他天冬氨酸蛋白酶（包括Cathepsin D，胃蛋白酶和肾素）抑制效果高50倍以上。Phase 1。 |
-
Journal of Agricultural and Food Chemistry, January 27, 2022, 1536-1546
-
Journal of Cell Biology, February 04, 2019, 644-663
-
Alzheimers & Dementia, August 12, 2019, 1183-1194
|
|
| S8173 |
Verubecestat (MK-8931) Trifluoroacetate
|
Verubecestat (MK-8931) Trifluoroacetate是一种有效的、选择性的beta-分泌酶的抑制剂、BACE1抑制剂。 |
-
Journal of Cerebral Blood Flow & Metabolism, 2023, 1235-1250
-
Alzheimers & Dementia: Translational Research & Clinical Interventions, 2022 Jul 14, e12317
-
Analyst, 2022, 10.1039/d2an00031h
|
|
| S8564 |
Verubecestat (MK-8931)
|
Verubecestat (MK-8931) 是一种有效的、选择性的beta-分泌酶（BACE）的抑制剂。 |
-
Alzheimers & Dementia: Translational Research & Clinical Interventions, July 14, 2022, 8(1):e12317
-
Int J Mol Sci, 2025, 26(8)3756
-
International Journal of Molecular Sciences, 2025, 3756
|
|
| S7731 |
AZD3839
|
AZD3839是一种有效的选择性BACE1抑制剂，Ki为26.1 nM，比作用于BACE2的选择性高14倍。Phase 1。
|
-
Elife, 2025, 13RP100968
-
Analyst, 2022, 10.1039/d2an00031h
-
Genome Med, 2021, 13(1):168
|
|
| S8193 |
Lanabecestat (AZD3293)
|
Lanabecestat (AZD3293, LY3314814) 是BACE抑制剂，Ki值为0.4 nM。 |
-
Analyst, 2022, 10.1039/d2an00031h
-
Communications Biology, 2020 Dec 1, 728
-
Alzheimers Res Ther, 2020, 26;12(1):63
|
|
| S4657 |
Eslicarbazepine Acetate
|
Eslicarbazepine Acetate (BIA 2093, Zebinix, Exalief, Stedesa, Aptiom) 是一种抗癫痫药物。 |
-
Cells, 2023, 1200
|
|
| S3326 |
Phytic acid dipotassium salt
|
Phytic acid dipotassium salt (Phytic acid potassium, IP6 (PS)) 是一种稻谷提取物和消化物中的内源性代谢物，可抑制 β-secretase 1 (BACE1)，其IC50值约为0.25 μM。 |
-
Analyst, 2022, 10.1039/d2an00031h
|
|
| S8600 |
Elenbecestat
|
Elenbecestat (E2609)是一种新型的BACE1抑制剂，在单次给药后能长效地减低血浆中β-淀粉样蛋白的水平。 |
-
EMBO Rep, 2025, 10.1038/s44319-025-00442-4
-
EMBO Reports, 2025, 2683-2714
|
|
| S3245 |
Nodakenetin
|
Nodakenetin (NANI) 是从Angelica decursiva中分离出的植物性香豆素，可抑制 α-glucosidase、PTP1B、rat lens aldose reductase (RLAR)、AChE、BChE 和 β-site amyloid precursor protein cleaving enzyme 1 (BACE1)。Nodakenetin 可改变 Bax 和 Bcl-2 的蛋白质表达，并促进线粒体凋亡。Nodakenetin 具有抗肿瘤活性。 |
|
|
| S6503 |
LX2343
|
LX2343是一种多靶点试剂，能够有效地减缓阿尔茨海默发病过程中多种异常指标。它是BACE1抑制剂，IC50为11.43±0.36 μM。 |
|
|
| S3835 |
Loganin
|
Loganin (Loganoside) is an iridoid glycoside first isolated from the seeds of Strychnos nux-vomica, a member of the Loganiaceae family. It is a non-competitive inhibitor of BACE1 with IC50 of 47.97 μM an also inhibits AChE and BChE with IC50 values of 3.95 μM and 33.02 μM, respectively. |
|
|
| S2156 |
LY2886721
|
LY2886721是BACE抑制剂，用于治疗阿尔茨海默症。Phase 1/2。 |
- Acta Neuropathol, 2025, 149(1):10
- Foods, 2024, 13(18)2858
- Stem Cell Reports, 2023, 18(7):1516-1533
|
|
| S1528 |
LY2811376
|
LY2811376是第一个口服有效的，非肽类β-secretase(BACE1)抑制剂，IC50为239 nM-249 nM，可以减少Aβ分泌，EC50为300 nM，作用于BACE1比作用于BACE2选择性高10倍，比作用于其他天冬氨酸蛋白酶（包括Cathepsin D，胃蛋白酶和肾素）抑制效果高50倍以上。Phase 1。 |
- Journal of Agricultural and Food Chemistry, January 27, 2022, 1536-1546
- Journal of Cell Biology, February 04, 2019, 644-663
- Alzheimers & Dementia, August 12, 2019, 1183-1194
|
|
| S8173 |
Verubecestat (MK-8931) Trifluoroacetate
|
Verubecestat (MK-8931) Trifluoroacetate是一种有效的、选择性的beta-分泌酶的抑制剂、BACE1抑制剂。 |
- Journal of Cerebral Blood Flow & Metabolism, 2023, 1235-1250
- Alzheimers & Dementia: Translational Research & Clinical Interventions, 2022 Jul 14, e12317
- Analyst, 2022, 10.1039/d2an00031h
|
|
| S8564 |
Verubecestat (MK-8931)
|
Verubecestat (MK-8931) 是一种有效的、选择性的beta-分泌酶（BACE）的抑制剂。 |
- Alzheimers & Dementia: Translational Research & Clinical Interventions, July 14, 2022, 8(1):e12317
- Int J Mol Sci, 2025, 26(8)3756
- International Journal of Molecular Sciences, 2025, 3756
|
|
| S7731 |
AZD3839
|
AZD3839是一种有效的选择性BACE1抑制剂，Ki为26.1 nM，比作用于BACE2的选择性高14倍。Phase 1。
|
- Elife, 2025, 13RP100968
- Analyst, 2022, 10.1039/d2an00031h
- Genome Med, 2021, 13(1):168
|
|
| S8193 |
Lanabecestat (AZD3293)
|
Lanabecestat (AZD3293, LY3314814) 是BACE抑制剂，Ki值为0.4 nM。 |
- Analyst, 2022, 10.1039/d2an00031h
- Communications Biology, 2020 Dec 1, 728
- Alzheimers Res Ther, 2020, 26;12(1):63
|
|
| S4657 |
Eslicarbazepine Acetate
|
Eslicarbazepine Acetate (BIA 2093, Zebinix, Exalief, Stedesa, Aptiom) 是一种抗癫痫药物。 |
- Cells, 2023, 1200
|
|
| S3326 |
Phytic acid dipotassium salt
|
Phytic acid dipotassium salt (Phytic acid potassium, IP6 (PS)) 是一种稻谷提取物和消化物中的内源性代谢物，可抑制 β-secretase 1 (BACE1)，其IC50值约为0.25 μM。 |
- Analyst, 2022, 10.1039/d2an00031h
|
|
| S8600 |
Elenbecestat
|
Elenbecestat (E2609)是一种新型的BACE1抑制剂，在单次给药后能长效地减低血浆中β-淀粉样蛋白的水平。 |
- EMBO Rep, 2025, 10.1038/s44319-025-00442-4
- EMBO Reports, 2025, 2683-2714
|
|
| S3245 |
Nodakenetin
|
Nodakenetin (NANI) 是从Angelica decursiva中分离出的植物性香豆素，可抑制 α-glucosidase、PTP1B、rat lens aldose reductase (RLAR)、AChE、BChE 和 β-site amyloid precursor protein cleaving enzyme 1 (BACE1)。Nodakenetin 可改变 Bax 和 Bcl-2 的蛋白质表达，并促进线粒体凋亡。Nodakenetin 具有抗肿瘤活性。 |
|
|
| S6503 |
LX2343
|
LX2343是一种多靶点试剂，能够有效地减缓阿尔茨海默发病过程中多种异常指标。它是BACE1抑制剂，IC50为11.43±0.36 μM。 |
|
|
| S3835 |
Loganin
|
Loganin (Loganoside) is an iridoid glycoside first isolated from the seeds of Strychnos nux-vomica, a member of the Loganiaceae family. It is a non-competitive inhibitor of BACE1 with IC50 of 47.97 μM an also inhibits AChE and BChE with IC50 values of 3.95 μM and 33.02 μM, respectively. |
|
|
