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Submit ReviewBMS 299897 is an orally active, potent γ-secretase inhibitor (IC50 = 12 nM). Inhibits Aβ40 and Aβ42 formation in vitro (IC50 values are 7.4 and 7.9 nM respectively) and reduces Aβ in the brain, plasma and cerebrospinal fluid in vivo. Exhibits no Notch toxicity. Brain penetrant.
BMS 299897 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 | 511.94 |
公式 | C24H21ClF3NO4S |
储存 | Store at -20°C |
纯度 | ≥98% (HPLC) |
CAS Number | 290315-45-6 |
PubChem ID | 11249248 |
InChI Key | IZAOBRWCUGOKNH-OAHLLOKOSA-N |
Smiles | FC1=CC=[C@@]([C@H](N(C3=CC(F)=CC=C3F)S(C2=CC=C(Cl)C=C2)(=O)=O)C)C(CCCC(O)=O)=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.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 51.19 | 100 | |
ethanol | 51.19 | 100 |
以下数据基于产品分子量 511.94。 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 | 1.95 mL | 9.77 mL | 19.53 mL |
5 mM | 0.39 mL | 1.95 mL | 3.91 mL |
10 mM | 0.2 mL | 0.98 mL | 1.95 mL |
50 mM | 0.04 mL | 0.2 mL | 0.39 mL |
参考文献是支持产品生物活性的出版物。
Barten et al (2005) Dynamics of β-Amyloid reductions in brain, cerebrospinal fluid, and plasma of β-amyloid precursor protein transgenic mice treated with a γ-secretase inhibitor. J.Pharmacol.Exp.Ther. 312 635 PMID: 15452193
Anderson et al (2005) Reductions in β-amyloid concentrations in vivo by the γ-secretase inhibitors BMS-289948 and BMS-299897. Biochem.Pharmacol. 69 689 PMID: 15670587
Goldstein et al (2007) Ex vivo occupancy of the γ-secretase inhibitors correlates with brain β-amyloid peptide reduction in Tg2576 mice. J.Pharmacol.Exp.Ther. 323 102 PMID: 17640949
If you know of a relevant reference for BMS 299897, please let us know.
关键词: BMS 299897, BMS 299897 supplier, BMS299897, gamma-secretase, inhibits, orally, active, inhibitors, g-secretase, beta-amyloid, b-amyloid, γ-secretase, β-amyloid, amyloidbeta, amyloidb, amyloidβ, Gamma-Secretase, Amyloid, Beta, Peptides, 2870, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 BMS 299897 的部分引用包括:
Liu et al (2018) APP upregulation contributes to retinal ganglion cell degeneration via JNK3. Cell Death Differ 25 661 PMID: 29238071
Pitt et al (2017) Neuroprotective astrocyte-derived Ins/IGF-1 stimulates endocytic processing and extracellular release of neuron-bound Aβ oligomers. Mol Biol Cell 28 2623 PMID: 28963439
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gamma -secretase (100 nM BMS 299897 and 250 nM DAPT)
Using more specific inhibitors, we ruled out the involvement of gamma -secretase (100 nM BMS 299897 and 250 nM DAPT) or matrix metalloproteinases 1, 2, 3, 7, 9, 14, and 17 (0.1–1 μM batimastat and marimastat), as their inhibitors failed to alter A beta O release