ARN2966APP expression modulator CAS# 102212-26-0 |
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Quality Control & MSDS
Number of papers citing our products
Chemical structure
3D structure
| Cas No. | 102212-26-0 | SDF | Download SDF |
| PubChem ID | 14936865 | Appearance | Powder |
| Formula | C12H12N2O | M.Wt | 200.24 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | DMSO : ≥ 43.4 mg/mL (216.74 mM) *"≥" means soluble, but saturation unknown. | ||
| Chemical Name | 2-(pyridin-2-ylmethylamino)phenol | ||
| SMILES | C1=CC=C(C(=C1)NCC2=CC=CC=N2)O | ||
| Standard InChIKey | GXJRVWZNMZGWAQ-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C12H12N2O/c15-12-7-2-1-6-11(12)14-9-10-5-3-4-8-13-10/h1-8,14-15H,9H2 | ||
| 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 | ARN2966 is a potent post-transcriptional modulator of APP expression; reduces expression of APP with resultant lower production of Aβ.
IC50 value:
Target: Aβ
This potent post-transcriptional modulation of APP expression differs from other mechanisms such as inhibition of secretases. Secretase inhibitors have been pursued as disease modifying strategies by a number of pharmaceutical firms but they have encountered numerous setbacks during clinical development. ARN2966 is non toxic, orally absorbable, blood-brain-barrier penetrable, and effective in vitro and in vivo. References: | |||||
ARN2966 Dilution Calculator
ARN2966 Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 4.994 mL | 24.97 mL | 49.9401 mL | 99.8801 mL | 124.8502 mL |
| 5 mM | 0.9988 mL | 4.994 mL | 9.988 mL | 19.976 mL | 24.97 mL |
| 10 mM | 0.4994 mL | 2.497 mL | 4.994 mL | 9.988 mL | 12.485 mL |
| 50 mM | 0.0999 mL | 0.4994 mL | 0.9988 mL | 1.9976 mL | 2.497 mL |
| 100 mM | 0.0499 mL | 0.2497 mL | 0.4994 mL | 0.9988 mL | 1.2485 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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ARN2966 is a potent post-transcriptional modulator of amyloid precursor protein (APP) expression in transfected CHO cells. The CHO cell can produce APP.[1]
APP is the amyloid precursor protein of Alzheimer’s disease. Alzheimer’s disease is a progressive dementia with the symptoms of neuronal degeneration, synaptic loss, and the deposition of amyloid fibrils in the brain. Ab protein is the major constituent of the amyloid . Then the Ab protein derives from the amyloid precursor protein (APP). It has been proved that APP can stimulate neurite outgrowth in vitro. [2]
The modulation of App expression of the ARN2966 functions as a post-transcriptional modulation,which is different from other mechanisms such as inhibition of secretases. ARN2966 showed dose dependant inhibition of Aß40 and Aß42 productions in APP751SW transfected CHO cells (IC50<1 mM for Aß40), along with lowering the level of APP and C83, and C99 peptides, while the level of APP mRNA was unaffected..[1]
There has been AD transgenic mice model proved ARN2966’s efficacy and tolerability in vivo. Through the treatment of ARN2966, the memory of mice has been improved and A load in the brain has been reduced.
References:
[1] Ayodeji Asuni ,Xu Kevin , etal. , An APP translation modulator ARN2966 reduces BETA-AMYLOID deposition and prevents memory deficits in ALZHEIMER'S DISEASE transgenic mice. Alzheimer's & Dementia: The Journal of the Alzheimer's Association, July 2012Volume 8, Issue 4, Supplement, Page S744 ;
[2]Williamson TG1, Mok SS, Henry A, etal. , Secreted glypican binds to the amyloid precursor protein of Alzheimer's disease (APP) and inhibits APP-induced neurite outgrowth. J Biol Chem. 1996 Dec 6;271(49):31215-21.
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