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Verubecestat

Cat. No. 7659 提交评论 说明书 / 分析证书（CoA） / 化学品安全技术说明书（SDS）
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说明： BACE1 and BACE2 inhibitor
化学名： N-[3-[(5R)-3-Amino-5,6-dihydro-2,5-dimethyl-1,1-dioxido-2H-1,2,4-thiadiazin-5-yl]-4-fluorophenyl]-5-fluoro-2-pyridinecarboxamide
纯度： ≥98% (HPLC)
说明书
引用文献
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生物活性 技术数据 溶解性 计算器 说明书 参考文献

生物活性 for Verubecestat

Verubecestat is a high affinity and selective β-secretase 1 (BACE1) and its homolog BACE2 inhibitor (Ki of 2.2 nM and 0.38 nM respectively). It exhibits no inhibition of cathepsin D, cathepsin E, pepsin, or renin. Verubecestat potently reduces Aβ40 formation in HEK293 APPSwe/Lon cells (IC50 = 2.1 nM). Verubecestat significantly lowers CSF and brain Aβ levels in rats. Orally bioavailable.

化合物库 for Verubecestat

Verubecestat is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。

技术数据 for Verubecestat

分子量 409.41
公式 C17H17F2N5O3S
储存 Store at -20°C
纯度 ≥98% (HPLC)
CAS Number 1286770-55-5
PubChem ID 51352361
InChI Key YHYKUSGACIYRML-KRWDZBQOSA-N
Smiles C[C@@]1(C2=CC(NC(=O)C3=CC=C(F)C=N3)=CC=C2F)CS(=O)(=O)N(C)C(N)=N1

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.

溶解性数据 for Verubecestat

溶剂 最高浓度 mg/mL 最高浓度 mM
溶解性
DMSO 40.94 100
ethanol 8.19 20

制备储备液 for Verubecestat

以下数据基于产品分子量 409.41。 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.

选择批次从而根据批次分子量重新计算:
浓度/溶剂体积/质量 1 mg 5 mg 10 mg
1 mM 2.44 mL 12.21 mL 24.43 mL
5 mM 0.49 mL 2.44 mL 4.89 mL
10 mM 0.24 mL 1.22 mL 2.44 mL
50 mM 0.05 mL 0.24 mL 0.49 mL

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参考文献 for Verubecestat

参考文献是支持产品生物活性的出版物。

Scott et al (2016) Discovery of the 3-imino-1,2,4-thiadiazinane 1,1-dioxide derivative Verubecestat (MK-8931) - A β-site amyloid precursor protein cleaving enzyme 1 inhibitor for the treatment of Alzheimer's disease. J.Med.Chem. 59 10435 PMID: 27933948

If you know of a relevant reference for Verubecestat, please let us know.

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关键词: Verubecestat, Verubecestat supplier, potent, selective, inhibitors, inhibits, beta-secretase, BACE1, BACE2, beta, amyloid, Alzheimers, disease, alzheimer's, Other, Proteases, Amyloid, Beta, Peptides, 7659, Tocris Bioscience

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