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Submit ReviewLY 2886721 Hydrochloride is a potent and selective β-secretase (BACE) inhibitor (IC50 values are 10.2 and 20.3 nM for human BACE2 and BACE1, respectively). Displays >5,000-fold selectivity for BACE over other proteases including cathepsin D, pepsin and renin. Inhibits Aβ1-40 and Aβ1-42 production in cells expressing mutated APP. Reduces hippocampal and cortical Aβ and sAPPβ levels in an Alzheimer's disease mouse model.
LY 2886721 Hydrochloride is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。
分子量 | 426.87 |
公式 | C18H16F2N4O2S.HCl |
储存 | Store at -20°C |
纯度 | ≥98% (HPLC) |
CAS Number | 1262036-49-6 |
PubChem ID | 50902942 |
InChI Key | JHHMCINLHBUFHB-GHDSXOKHSA-N |
Smiles | [H][C@@]12COC[C@]1(C3=CC(NC(C4=CC=C(C=N4)F)=O)=CC=C3F)N=C(SC2)N.Cl |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 42.69 | 100 |
以下数据基于产品分子量 426.87。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 2.34 mL | 11.71 mL | 23.43 mL |
5 mM | 0.47 mL | 2.34 mL | 4.69 mL |
10 mM | 0.23 mL | 1.17 mL | 2.34 mL |
50 mM | 0.05 mL | 0.23 mL | 0.47 mL |
参考文献是支持产品生物活性的出版物。
May et al (2015) The potent BACE1 inhibitor LY2886721 elicits robust central Aβ pharmacodynamic responses in mice, dogs and humans. J.Neurosci. 35 1199 PMID: 25609634
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