E 2012γ--Secretase modulator CAS# 870843-42-8 |
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Quality Control & MSDS
3D structure
Package In Stock
Number of papers citing our products
| Cas No. | 870843-42-8 | SDF | Download SDF |
| PubChem ID | 11560787 | Appearance | Powder |
| Formula | C25H26FN3O2 | M.Wt | 419.49 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | DMSO : ≥ 50 mg/mL (119.19 mM) *"≥" means soluble, but saturation unknown. | ||
| Chemical Name | (3E)-1-[(1S)-1-(4-fluorophenyl)ethyl]-3-[[3-methoxy-4-(4-methylimidazol-1-yl)phenyl]methylidene]piperidin-2-one | ||
| SMILES | CC1=CN(C=N1)C2=C(C=C(C=C2)C=C3CCCN(C3=O)C(C)C4=CC=C(C=C4)F)OC | ||
| Standard InChIKey | PUOAETJYKQITMO-LANLRWRYSA-N | ||
| Standard InChI | InChI=1S/C25H26FN3O2/c1-17-15-28(16-27-17)23-11-6-19(14-24(23)31-3)13-21-5-4-12-29(25(21)30)18(2)20-7-9-22(26)10-8-20/h6-11,13-16,18H,4-5,12H2,1-3H3/b21-13+/t18-/m0/s1 | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | E 2012 is a potent γ-secretase modulator.
IC50 value:
Target: γ-secretase
In the present study, 9 dogs were treated with a single dose of the γ-secretase modulator E2012, the γ-secretase inhibitor LY450139, or vehicle with a dosing interval of 1 week. The isoform Aβ(1-37) was significantly increased in a dose-dependent manner in response to treatment with E2012, while Aβ(1-39), Aβ(1-40) and A(1-42) decreased [1].
E2012, a gamma secretase modulator without affecting Notch processing, aimed at Alzheimer's disease by reduction of amyloid β-42, induced cataract following repeated doses in the rat.E2012 inhibits 3β-hydroxysterol Δ24-reductase (DHCR24) at the final step in the cholesterol biosynthesis. In vivo lenticular concentration of E2012 after 13-week repeated dose with cataract was well above those where inhibition was observed in vitro.E2012 induces cataract in the rat by inhibiting DHCR24 at the final step of cholesterol synthesis with associated elevation in desmosterol within the lens, preceded by desmosterol changes that would serve as a predictive safety biomarker for lenticular opacity [2]. References: | |||||
E 2012 Dilution Calculator
E 2012 Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 2.3838 mL | 11.9192 mL | 23.8385 mL | 47.6769 mL | 59.5962 mL |
| 5 mM | 0.4768 mL | 2.3838 mL | 4.7677 mL | 9.5354 mL | 11.9192 mL |
| 10 mM | 0.2384 mL | 1.1919 mL | 2.3838 mL | 4.7677 mL | 5.9596 mL |
| 50 mM | 0.0477 mL | 0.2384 mL | 0.4768 mL | 0.9535 mL | 1.1919 mL |
| 100 mM | 0.0238 mL | 0.1192 mL | 0.2384 mL | 0.4768 mL | 0.596 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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E 2012 is γ-secretase inhibitor.
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Assessment of the Activity of Tigecycline against Gram-Positive and Gram-Negative Organisms Collected from Italy between 2012 and 2014, as Part of the Tigecycline Evaluation and Surveillance Trial (T.E.S.T.).[Pubmed:27898030]
Pharmaceuticals (Basel). 2016 Nov 26;9(4). pii: ph9040074.
As part of the Tigecycline Evaluation and Surveillance Trial (T.E.S.T) we report the in vitro activity of tigecycline and its comparators against Gram-negative and Gram-positive organisms collected from Italian centers between 2012 and 2014. Minimum inhibitory concentrations were determined according to the broth microdilution methodology of the Clinical and Laboratory Standards Institute, and antimicrobial resistance was determined using the European Committee on Antimicrobial Susceptibility Testing interpretive criteria. Among the Enterobacteriaceae, 31% of Escherichia coli isolates, 22% of Klebsiella pneumoniae, and 1% of Klebsiella oxytoca were extended-spectrum beta-lactamase producers (ESBLs). Resistance rates among ESBL-K. pneumoniae and ESBL-E. coli to meropenem were 24% and <1%, respectively. Thirty-seven percent of K. pneumoniae were multidrug resistant (MDR) strains. Resistance rates among isolates of Acinetobacter baumannii to amikacin, levofloxacin and meropenem were between 84% and 94%. Eighty percent of A. baumannii isolates were MDR strains. Methicillin-resistant Staphylococcus aureus (MRSA) accounted for 38% of S. aureus isolates. No isolates of MRSA were resistant to linezolid, tigecycline or vancomycin. Antimicrobial resistance remains a problem in Italy with increasing numbers of MDR organisms. Despite high levels, MRSA rates appear to be stabilising. Tigecycline retains its in vitro activity against the majority of organisms, including those with multidrug resistance.
Changing Perceptions of Harm of E-Cigarettes Among U.S. Adults, 2012-2015.[Pubmed:28341303]
Am J Prev Med. 2017 Mar;52(3):331-338.
INTRODUCTION: Although the impact of long-term use of electronic cigarettes (e-cigarettes) on health is still unknown, current scientific evidence indicates that e-cigarettes are less harmful than combustible cigarettes. The study examined whether perceived relative harm of e-cigarettes and perceived addictiveness have changed during 2012-2015 among U.S. adults. METHODS: Data were from Tobacco Products and Risk Perceptions surveys of probability samples representative of U.S. adults in 2012, 2014, and 2015. Changes over time in perceived harmfulness of e-cigarettes were examined using pairwise comparisons of proportions and multinomial logistic regression analysis. Analyses were conducted in January 2016. RESULTS: Whereas 11.5% and 1.3% of adults perceived e-cigarettes to have about the same level of harm and to be more harmful than cigarettes, respectively, in 2012, 35.7% and 4.1% did so in 2015. The proportion of adults who thought e-cigarettes were addictive more than doubled during 2012-2015 (32.0% in 2012 vs 67.6% in 2015). Compared with 2012, the odds of perceiving e-cigarettes to be equally or more harmful (than to be less harmful) doubled (95% CI=1.64, 2.41) in 2014, and tripled (95% CI=2.60, 3.81) in 2015. CONCLUSIONS: There is an increase in the proportion of U.S. adults who misperceive the harm of e-cigarettes and consider them to be as harmful as combustible cigarettes. The study highlights the need to design public health messages that accurately interpret the scientific data on the potential harm of e-cigarettes and clearly differentiate the absolute from the relative harm of e-cigarettes.
Erratum: Spatiotemporal bounded noises and transitions induced by them in solutions of the real Ginzburg-Landau model [Phys. Rev. E 86, 021118 (2012)].[Pubmed:27967005]
Phys Rev E. 2016 Nov;94(5-2):059905.
This corrects the article DOI: 10.1103/PhysRevE.86.021118.
