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Submit ReviewMRK 560
说明： γ-secretase inhibitor; attenuates amyloid plaque deposition
化学名： N-[cis-4-[(4-Chlorophenyl)sulfonyl]-4-(2,5-difluorophenyl)cyclohexyl]-1,1,1-trifluoromethanesulfonamide
纯度： ≥99% (HPLC)
生物活性 for MRK 560
MRK 560 is a γ-secretase inhibitor, which selectively inhibits proteolytic cleavage of amyloid precursor protein (APP) over the Notch pathway. MRK 560 reduces levels of Aβ in vitro (inhibits Aβ40 and Aβ42 in SH-SY5Y neuroblastoma cells with an IC50 of 0.65 nM) and attenuates plaque deposition. This compound is orally bioavailable.
许可信息
Manufactured and sold under license from Merck & Co., Inc. for use solely for preclinical research purposes (ie: not for administration to or other use in humans).
Extrernal Portal Information for MRK 560
The Chemical Probes webpages of the Structural Genomics Consortium are a portal that offers independent guidance on the selection and/or application of small molecules for research. The use of MRK 560 is reviewed.
化合物库 for MRK 560
MRK 560 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 MRK 560
| 分子量 | 517.92 |
| 公式 | C19H17ClF5NO4S2 |
| 储存 | Store at +4°C |
| 纯度 | ≥99% (HPLC) |
| CAS Number | 677772-84-8 |
| PubChem ID | 11577204 |
| InChI Key | WDZVWDXOIGQJIO-UJKQEGAGSA-N |
| Smiles | FC1=CC(=C(F)C=C1)[C@]1(CC[C@@H](CC1)N[S](=O)(=O)C(F)(F)F)[S](=O)(=O)C1=CC=C(Cl)C=C1 |
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 MRK 560
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 51.79 | 100 | |
| ethanol | 25.9 | 50 |
制备储备液 for MRK 560
以下数据基于产品分子量 517.92。 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 | 1.93 mL | 9.65 mL | 19.31 mL |
| 5 mM | 0.39 mL | 1.93 mL | 3.86 mL |
| 10 mM | 0.19 mL | 0.97 mL | 1.93 mL |
| 50 mM | 0.04 mL | 0.19 mL | 0.39 mL |
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产品说明书 for MRK 560
参考文献 for MRK 560
参考文献是支持产品生物活性的出版物。
Best et al (2006) In vivo characterization of Aβ(40) changes in brain and cerebrospinal fluid using the novel γ-secretase inhibitor N-[cis-4-[(4-chlorophenyl)sulfonyl]-4-(2,5-difluorophenyl)cyclohexyl]-1,1,1-trifluoromethanesulfonamide (MRK-560) J.Pharm.Exp.Ther. 317 786 PMID: 16443723
Best et al (2007) The novel γ-secretase inhibitor N-[cis-4-[(4-chlorophenyl)sulfonyl]-4-(2,5-difluorophenyl)cyclohexyl]-1,1,1-trifluoromethanesulfonamide (MRK-560) reduces amyloid plaque deposition without evidence of Notch-related pathology in the T J.Pharm.Exp.Ther. 320 552 PMID: 17099072
If you know of a relevant reference for MRK 560, please let us know.
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关键词: MRK 560, MRK 560 supplier, MRK560, gamma-secretase, inhibitor, g-secretase, inhibitors, inhibits, secretases, amyloidbeta, amyloidb, amyloidβ, Gamma-Secretase, Amyloid, Beta, Peptides, 4000, Tocris Bioscience
3 篇 MRK 560 的引用文献
引用文献是使用了 Tocris 产品的出版物。 MRK 560 的部分引用包括：
Singh et al (2014) GSI promotes vincristine-induced apoptosis by enhancing multi-polar spindle formation. Cell Cycle 13 157 PMID: 24200971
Qi et al (2014) Longitudinal testing of hippocampal plasticity reveals the onset and maintenance of endogenous human Aβ-induced synaptic dysfunction in individual freely behaving pre-plaque transgenic rats: rapid reversal by anti-Aβ agents. Acta Neuropathol Commun 2 175 PMID: 25540024
Lariosa-Willingham et al (2016) Development of a central nervous system axonal myelination assay for high throughput screening. BMC Neurosci 17 16 PMID: 27103572
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