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Submit ReviewAvagacestat
说明： Highly potent γ-secretase inhibitor; orally bioavailable
别名： BMS-708163
化学名： (2R)-2-[[(4-Chlorophenyl)sulfonyl][[2-fluoro-4-(1,2,4-oxadiazol-3-yl)phenyl]methyl]amino]-5,5,5-trifluoropentanamide
纯度： ≥98% (HPLC)
生物活性 for Avagacestat
Avagacestat is a highly potent γ-secretase inhibitor (Aβ40 IC50 = 0.3 nM). Exhibits >137-fold selectivity for amyloid-β precursor protein (APP) processing over Notch. Reduces plasma and brain Aβ40 and Aβ42 levels in vivo. Orally bioavailable.
化合物库 for Avagacestat
Avagacestat 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 Avagacestat
| 分子量 | 520.89 |
| 公式 | C20H17ClF4N4O4S |
| 储存 | Store at +4°C |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 1146699-66-2 |
| PubChem ID | 46883536 |
| InChI Key | XEAOPVUAMONVLA-QGZVFWFLSA-N |
| Smiles | NC([C@H](N(S(=O)(C1=CC=C(C=C1)Cl)=O)CC2=C(C=C(C3=NOC=N3)C=C2)F)CCC(F)(F)F)=O |
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 Avagacestat
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 52.09 | 100 | |
| ethanol | 10.42 | 20 |
制备储备液 for Avagacestat
以下数据基于产品分子量 520.89。 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 | 1.92 mL | 9.6 mL | 19.2 mL |
| 5 mM | 0.38 mL | 1.92 mL | 3.84 mL |
| 10 mM | 0.19 mL | 0.96 mL | 1.92 mL |
| 50 mM | 0.04 mL | 0.19 mL | 0.38 mL |
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产品说明书 for Avagacestat
参考文献 for Avagacestat
参考文献是支持产品生物活性的出版物。
Gillman et al (2010) Discovery and evaluation of BMS-708163, a potent, selective and orally bioavailable γ-secretase inhibitor. ACS Med.Chem.Lett. 1 120 PMID: 24900185
Albright et al (2013) Pharmacodynamics of selective inhibition of γ-secretase by avagacestat. J.Pharmacol.Exp.Ther. 344 686 PMID: 23275065
If you know of a relevant reference for Avagacestat, please let us know.
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关键词: Avagacestat, Avagacestat supplier, gamma, γ, secretase, inhibitors, inhibits, Abeta, AB, Aβ40, 42, amyloid-β, precursor, protein, APP, processing, highly, potent, BMS-708163, Gamma-Secretase, Amyloid, Beta, Peptides, 6363, Tocris Bioscience
1 篇 Avagacestat 的引用文献
引用文献是使用了 Tocris 产品的出版物。 Avagacestat 的部分引用包括：
Wulf et al (2021) Roles for ADAM17 in TNF-R1 Mediated Cell Death and Survival in Human U937 and Jurkat Cells. Cells 10 PMID: 34831323
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