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首页-小分子抑制剂&激动剂-Metabolic Enzyme/Protease-Beta-secretase (BACE)-Atabecestat
Atabecestat

Chemical Structure : Atabecestat

CAS No.: 1200493-78-2

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Atabecestat (JNJ-54861911;JNJ54861911)

货号: PC-60507Not For Human Use, Lab Use Only.

Atabecestat (JNJ-54861911) is a potent, selective, brain penetrable and orally bioavailable BACE1 inhibitor with IC50 of 9.8 nM in HTRF assays, inhibits BACE2 (IC50=5.6 nM) with comparable potency as for BACE1.

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5 mg ￥3280 In stock
10 mg ￥5280 In stock
25 mg ￥8980 In stock
50 mg Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Atabecestat (JNJ-54861911) is a potent, selective, brain penetrable and orally bioavailable BACE1 inhibitor with IC50 of 9.8 nM in HTRF assays, inhibits BACE2 (IC50=5.6 nM) with comparable potency as for BACE1.
Atabecestat (JNJ-54861911) pontently inhibits levels of secreted Aβ40 in human APP-transfected human neuroblastoma (SH-SY5Y) cells with IC50 of 1.1 nM.
Atabecestat (JNJ-54861911) shows comparable potency for mouse and dog BACE1 with IC50 values of 9.7 and 12 nM, respectively.
Atabecestat (JNJ-54861911) is extremely selective over CatD and CatE (IC50 = >100 μM).
Atabecestat (JNJ-54861911) demonstrated robust and dose-dependent Aβ reduction and showed sufficient safety margins in preclinical models.

物理化学性质&存储条件

分子量 367.4
分子式 C18H14FN5OS
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

(S)-N-(3-(2-amino-4-methyl-4H-1,3-thiazin-4-yl)-4-fluorophenyl)-5-cyanopicolinamide

参考文献

1. Timmers M, et al. Alzheimers Dement (N Y). 2016 Aug 24;2(3):202-212.

2. Timmers M, et al. J Alzheimers Dis. 2017;56(4):1437-1449.

3. Timmers M, et al. J Clin Pharmacol. 2018 Mar 5. doi: 10.1002/jcph.1087. 

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