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首页-小分子抑制剂&激动剂-Metabolic Enzyme/Protease-Beta-secretase (BACE)-PF-06751979
PF-06751979

Chemical Structure : PF-06751979

CAS No.: 1818339-66-0

PF-06751979 (PF06751979)

货号: PC-63290Not For Human Use, Lab Use Only.

PF-06751979 is a potent, selective, brain penetrant BACE1 inhibitor with binding IC50 of 7.3, 27-fold selectivity over BACE2.

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10 mg ¥5580 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

PF-06751979 is a potent, selective, brain penetrant BACE1 inhibitor with binding IC50 of 7.3, 27-fold selectivity over BACE2.
PF-06751979 shows BACE1 inhibition and sAPPβ production in whole-cell assay with IC50 of 5.1 and 5 nM.
PF-06751979 displays excellent brain penetration, potent in vivo efficacy, and broad selectivity over related aspartyl proteases including BACE2; demonstrates potent and dose-dependent Aβ lowering in human CSF with lacking hypopigmentation compared with AZD3239.

物理化学性质&存储条件

分子量 455.499
分子式 C18H19F2N5O3S2
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

N-(2-((4aR,6S,8aR)-2-amino-6-methyl-4,4a,5,6-tetrahydropyrano[3,4-d][1,3]thiazin-8a(8H)-yl)thiazol-4-yl)-5-(difluoromethoxy)picolinamide

参考文献

1. O'Neill BT, et al. J Med Chem. 2018 Apr 3. doi: 10.1021/acs.jmedchem.8b00246.

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