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Begacestat is a γ-secretase inhibitor; selectively inhibits cleavage of amyloid precursor protein (APP) over Notch. Lowers levels of Aβ42 and Aβ40 (EC50 values are 12.4 and 14.8 nM respectively in cells expressing human recombinant APP). Orally active.
Sold for research purposes under agreement from Pfizer Inc.
分子量 | 391.74 |
公式 | C9H8ClF6NO3S2 |
储存 | Store at +4°C |
纯度 | ≥98% (HPLC) |
CAS Number | 769169-27-9 |
PubChem ID | 11269353 |
InChI Key | PSXOKXJMVRSARX-SCSAIBSYSA-N |
Smiles | ClC1=CC=C(S(N[C@H](CO)C(C(F)(F)F)C(F)(F)F)(=O)=O)S1 |
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.
参考文献是支持产品生物活性的出版物。
Mayer et al (2008) Discovery of begacestat, a Notch-1-sparing gamma secretase inhibitor for the treatment of Alzheimer's disease. J.Med.Chem. 51 7348 PMID: 19012391
Martone et al (2009) Begacestat (GSI-953): a novel, selective thiophene sulfonamide inhibitor of amyloid precursor protein γ-secretase for the treatment of Alzheimer's disease. J.Pharmacol.Exp.Ther. 331 598 PMID: 19671883
关键词: Begacestat, Begacestat supplier, GSI953, Begacestat, pfizer, gamma, gamma-secretase, γ, g-secretase, inhibitors, inhibits, APP, amyloid, precursor, proteins, notch, AB40, Abeta40, Aβ40, AB42, Abeta42, Aβ42, amyloidbeta, amyloidb, amyloidβ, GSI-953, Gamma-Secretase, Amyloid, Beta, Peptides, 4283, Tocris Bioscience
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