21
8
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T12188 |
NB-360
|
BACE | Neuroscience |
NB-360 是一种有效的脑穿透性 BACE1 和 BACE2 抑制剂,对小鼠和人源 BACE1 和 BACE2 的 IC50 分别为 5、5 和 6 nM。 NB-360 对相关的天冬氨酰蛋白酶、胃蛋白酶、组织蛋白酶 E 和组织蛋白酶 D 具有出色的特异性。 | |||
T2639 |
LY2811376
|
Beta Amyloid; Beta-Secretase; BACE | Neuroscience |
LY2811376 是可口服的非肽段β-secretase (BACE1)抑制剂,IC50=239 nM-249 nM,能够降低 Aβ 蛋白的分泌,EC50=300 nM。 | |||
T13253 |
Umibecestat
CNP520 |
BACE | Neuroscience |
Umibecestat 是一种β-位点淀粉样前体蛋白裂解酶-1 (BACE-1) 抑制剂,对人 BACE-1 和小鼠 BACE-1 的 IC50 分别为 11 nM 和 10 nM,可用于阿尔茨海默病的研究。 | |||
T6058 |
LY2886721
|
Beta-Secretase; BACE | Neuroscience |
LY2886721 是选择性的,口服活性的 β 位淀粉样蛋白前体蛋白裂解酶 1 抑制剂,对重组人 BACE1的 IC50=20.3 nM。它对 BACE1的选择性高于对组织蛋白酶 D、胃蛋白酶、肾素的选择性,但缺乏对 BACE2的选择性。它可透过血脑屏障,并可用于研究阿尔茨海默氏病。 | |||
T11175 |
Elenbecestat
E2609 |
Beta-Secretase; BACE | Neuroscience |
Elenbecestat (E2609) 是一种高效、有口服活性的,能透过 CNS 的 BACE-1抑制剂,它有用于阿尔茨海默病 (AD) 的研究潜力。 | |||
T6772 |
AZD3839 free base
AZD3839 |
Beta-Secretase; BACE | Neuroscience |
AZD3839 free base 是一种具有口服活性的、选择性的、可透过大脑屏障的BACE1抑制剂 (Ki=26 nM),对 BACE2 和组织蛋白酶 D 的选择性分别为 14 倍和 >1000 倍。在小鼠、豚鼠和非人灵长类动物中,它剂量和时间依赖性的降低血浆、脑和脑脊液 Aβ 水平,可用于研究阿尔茨海默病。 | |||
T4398 |
LX2343
|
Beta Amyloid; Beta-Secretase; BACE; PI3K; Autophagy | Autophagy; Neuroscience; PI3K/Akt/mTOR signaling |
LX2343 是一种非 ATP 竞争性 PI3K 抑制剂,IC50 为 15.99±3.23 μM。它是一种 BACE1 酶抑制剂,IC50 值为 11.43±0.36 μM。它在促进 Aβ 清除中刺激自噬。 | |||
T7011 |
Verubecestat
MK-8931,维罗司他 |
Beta-Secretase; BACE | Neuroscience |
Verubecestat (MK-8931) 是一种高亲和力的、具有口服活性的BACE1和BACE2抑制剂,Ki 分别为 2.2 nM 和 0.38 nM。它可以有效降低 Aβ40,并具有潜力用于阿尔茨海默氏病。 | |||
T3285 |
Eslicarbazepine Acetate
Zebinix,Aptiom,BIA 2-093,Exalief,艾司利卡西平醋酸酯,Stedesa |
Beta-Secretase; Sodium Channel | Membrane transporter/Ion channel; Neuroscience |
Eslicarbazepine Acetate (Zebinix) 是一种抗癫痫药物。Eslicarbazepine acetate 也是 β-内分泌酶(β-Secretase)和电压门控钠离子通道的双抑制剂。 | |||
T13434 |
β-Secretase Inhibitor IV
|
Others | Others |
β-Secretase Inhibitor IV is a potent, cell-active inhibitor of BACE-1(IC50s of 15.6 and 16.3nM under BACE-1 concentrations of 2 nM and 100 pM, respectively). | |||
T40260 |
β-Secretase Inhibitor II
|
||
β-Secretase Inhibitor II is a tripeptide aldehyde compound that acts as an inhibitor of β-Secretase. It exhibits a simple structure and has an inhibitory potency of IC50 = 700 nM against total Aβ and IC50 = 2.5 μM specifically against Aβ 1-42. This compound is particularly useful in research related to Alzheimer's disease. | |||
T3161 |
β-Secretase inhibitor-STA
|
Beta-Secretase | Neuroscience |
BACE-IN-1 是淀粉样前体蛋白 β-分泌酶抑制剂。 | |||
T39251 |
β-Secretase Inhibitor I
|
||
β-Secretase Inhibitor I is a highly potent inhibitor of the β-secretase enzyme. This compound exhibits exceptional inhibitory activity while also demonstrating a significant reduction in cardiovascular and liver toxicity. | |||
T11362 |
gamma-Secretase Modulators
γ-Secretase Modulators,Amyloid-β production inhibitor |
Others | Others |
gamma-Secretase Modulators serves as a useful treatment for Alzheimer's disease by inhibiting the production of Amyloid-β. Specifically, it acts as a gamma-Secretase Modulators with an IC50 value. | |||
T83616 |
SEW06622
|
BACE; AChE | Neuroscience |
SEW06622 是一种有效的 乙酰胆碱酯酶(AChE)和β-分泌酶-1(BACE-1)抑制剂,是治疗阿尔茨海默病的潜在候选化合物。 | |||
T6870 |
L-685458
L-685,458 |
Apoptosis; Gamma-secretase | Apoptosis; Neuroscience; Proteases/Proteasome; Stem Cells |
L-685458 (L-685,458) 是一种过渡状态模拟 γ-分泌酶抑制剂,抑制淀粉样 β-蛋白前体 γ-分泌酶活性,选择性高于其他检测的天冬氨酸蛋白酶 50-100 倍。它抑制 γ-分泌酶介导的 APP-C99 和 Notch-100 的裂解,可研究阿尔茨海默病和癌症。 | |||
T28390 |
PF9238
PF 9238,PF-9238 |
||
PF9238 is an inhibitor of beta-secretase I. PF9238 has a CatD potency of 12 uM in vivo. | |||
T24924 |
Umibecestat HCl (1387560-01-1 free base)
CNP 520,Umibecestat HCl,Umibecestat hydrochloride,CNP520,CNP-520 |
||
Umibecestat is a beta-secretase inhibitor. CNP520 has a selectivity, pharmacodynamics, and distribution profile suitable for AD prevention studies. | |||
T70104 |
Verubecestat tosylate
|
||
Verubecestat, also known as MK-8931 or SCH 900931, is a potent and selective beta-secretase inhibitor, and BACE1 protein inhibitor or Beta-site APP-cleaving enzyme 1 inhibitor. Verubecestat is a promising novel therapeutic drug candidate in Alzheimer's disease. Verubecestat reduced Aβ cerebral spinal fluids (CSF) levels up to 92% and was well tolerated by patients. | |||
T71899 |
Verubecestat TFA
|
||
Verubecestat, also known as MK-8931 or SCH 900931, is a potent and selective beta-secretase inhibitor, and BACE1 protein inhibitor or Beta-site APP-cleaving enzyme 1 inhibitor. Verubecestat is a promising novel therapeutic drug candidate in Alzheimer's disease. Verubecestat reduced Aβ cerebral spinal fluids (CSF) levels up to 92% and was well tolerated by patients. | |||
T69664 | Umibecestat HCl | ||
Umibecestat, also known as CNP-520, is a beta-secretase inhibitor and is a drug candidate for prevention trials in Alzheimer's disease. CNP520 has a selectivity, pharmacodynamics, and distribution profile suitable for AD prevention studies. CNP520 reduced brain and cerebrospinal fluid (CSF) Aβ in rats and dogs, and Aβ plaque deposition in APP-transgenic mice. CNP520 reduces Aβ load and neuroinflammation in APP‐transgenic mice |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T5S2361 |
Epiberberine
|
ERK; Beta-Secretase; MEK; BACE; AMPK; AChR; AChE | Chromatin/Epigenetic; MAPK; Neuroscience; PI3K/Akt/mTOR signaling |
Epiberberine 是一种从黄连中得到的生物碱,是AChE 和BChE 抑制剂,和非竞争性BACE1抑制剂。在 3T3-L1 细胞分化早期,它能够下调 Raf/MEK1/2/ERK1/2 和 AMPKα/Akt 信号通路。它具有抗氧化作用,能够清除 ONOO-,可用于阿尔滋海默症和糖尿病的研究。 | |||
T3769 |
Tenuifolin
|
Others; Beta-Secretase; AChE | Neuroscience; Others |
Tenuifolin 是一种从远志中分离出的三萜,能够抑制β-secretase 以减少 Aβ 蛋白分泌,具有神经保护作用。 它可通过降低 AChE 活性来改善衰老小鼠的学习和记忆能力,有潜力用于阿尔茨海默氏病的研究。 | |||
TN2190 |
Scoulerine
|
Apoptosis; Beta-Secretase; BACE; Parasite | Apoptosis; Microbiology/Virology; Neuroscience |
Scoulerine 是抗有丝分裂化合物。它抑制细胞增殖,阻止细胞周期,并诱导癌细胞凋亡。它也是BACE1(淀粉样前体蛋白裂解酶 1) 的抑制剂。 | |||
T8179 |
Aloeresin D
芦荟新甙D,芦荟新苷 D |
Beta-Secretase; BACE | Neuroscience |
Aloeresin D 是一种从芦荟中分离得到的色原酮苷,能够抑制 β-分泌酶活性,IC50=39 μM。 | |||
T2S1181 |
Aloenin
Aloenin A,Aloearbonaside,芦荟宁 |
Beta-Secretase; AChR | Neuroscience |
Aloenin (Aloenin A) A 是一种具有清除过氧自由基作用的天然产物,对 β-分泌酶 (BACE) 具有中等抑制活性。 | |||
TN2217 |
Sophoflavescenol
槐苦参醇,槐黄醇 |
Others; Beta-Secretase; BACE; PDE; AChR; AChE | Metabolism; Neuroscience; Others |
Sophoflavescenol 是异戊烯基黄酮类化合物,能够抑制PDE5的活性,IC50=0.013 μM。它也抑制 RLAR,HRAR,BACE1,AChE 和 BChE,IC50值分别为 0.30 µM,0.17 µM,10.98 µM,8.37 µM 和 8.21 µM。 | |||
T8306 |
Epiberberine chloride
表小檗碱氯化物,Epiberberine (chloride),盐酸表小檗碱 |
Reactive Oxygen Species; Beta-Secretase; BACE; AChR; AChE | Immunology/Inflammation; Metabolism; Neuroscience; NF-κB |
Epiberberine chloride (Epiberberine (chloride)) 是一种从黄连中得到的生物碱,是一种AChE 和BChE 抑制剂,和非竞争性的BACE1抑制剂。它具有抗氧化作用,能够清除 ONOO-,可用于研究阿尔滋海默症和糖尿病。 | |||
T3682 |
(-)-Catechin gallate
(-)-Catechin 3-O-gallate,儿茶素没食子酸酯,几茶素没食子酸酯,(-)-Catechin 3-gallate |
Others; COX | Immunology/Inflammation; Neuroscience; Others |
(-)-Catechin gallate ((-)-Catechin 3-O-gallate) 是绿茶儿茶素中的微量组分,可抑制COX-1和COX-2活性。它抑制人 Beta-secretase,对氯喹敏感的恶性疟原虫 NF54 和耐氯喹的恶性疟原虫 K1 具有抗疟原虫活性。 |