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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.
|Storage||Store at -20°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 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.
|Concentration / Solvent Volume / Mass||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|
References are publications that support the biological activity of the product.
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
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Keywords: 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
2 Citations for BMS 299897
Citations are publications that use Tocris products. Selected citations for BMS 299897 include:
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
Liu et al (2018) APP upregulation contributes to retinal ganglion cell degeneration via JNK3. Cell Death Differ 25 661 PMID: 29238071
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Reviews for BMS 299897
Average Rating: 5 (Based on 1 Review.)
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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
Literature in this Area
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Alzheimer's disease (AD) is a degenerative brain disease and the most common cause of dementia, affecting approximately 47 million people worldwide. Updated in 2015, this poster summarizes the structural and functional changes observed in the progression of this neurodegenerative disease, as well as classic AD drug targets.