| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
Purity: ≥98%
| Targets |
ARN2966 targets the expression of amyloid precursor protein (APP), the precursor to amyloid-β (Aβ) peptides that aggregate to form plaques in Alzheimer's disease. It acts as a post-transcriptional modulator of APP expression, reducing APP levels without affecting cell viability. By lowering APP expression, it reduces the production of Aβ peptides, which are neurotoxic.
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| ln Vitro |
In vitro, ARN2966 reduces levels of APP and its intracellular C-terminal fragments α-CTF and β-CTF in CHO APP751SW cells when used at a concentration of 10 μM. It is a potent post-transcriptional modulator of APP expression in transfected CHO cells that produce APP. It reduces APP expression with resultant lower production of Aβ.
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| ln Vivo |
In vivo, ARN2966 improves memory and reduces Aβ in Alzheimer's disease transgenic mice. It is orally active and blood-brain barrier penetrant. It is non-toxic and effective in vivo. These results demonstrate its potential as a therapeutic agent for Alzheimer's disease.
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| Enzyme Assay |
In vitro APP expression assays for ARN2966 are performed using CHO cells stably expressing APP751SW. Cells are cultured in appropriate media and treated with ARN2966 at various concentrations (e.g., 10 μM) for a defined period. APP levels, as well as α-CTF and β-CTF levels, are measured by Western blot. Aβ levels in the culture medium are measured by ELISA.
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| Cell Assay |
In vitro cell-based assays for ARN2966 are performed using CHO APP751SW cells. Cells are cultured in appropriate media and treated with ARN2966 at various concentrations. Cell viability is assessed by MTT assays to confirm lack of toxicity. APP and Aβ levels are measured by Western blot and ELISA, respectively. The effects on APP processing and Aβ production are assessed.
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| Animal Protocol |
In vivo animal studies for ARN2966 are conducted in transgenic mouse models of Alzheimer's disease (e.g., APP/PS1 mice). The compound is administered orally. Cognitive function is assessed using behavioral tests such as the Morris water maze or novel object recognition. Aβ levels in the brain are measured by ELISA or immunohistochemistry.
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| ADME/Pharmacokinetics |
ARN2966 is orally active and blood-brain barrier penetrant. Specific pharmacokinetic properties, such as half-life and bioavailability, are not extensively detailed in the available literature. As a small molecule with a molecular weight of 200.24 g/mol, it is expected to have good oral bioavailability and brain penetration. It is soluble in DMSO.
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| Toxicity/Toxicokinetics |
ARN2966 is non-toxic. In cell-based assays, it shows no cytotoxicity at effective concentrations. As a research compound, it is intended for laboratory use only and is not for human therapeutic use. Standard safety precautions should be followed when handling this compound.
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| References |
:http://arianeurosciences.com/science.html
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| Additional Infomation |
ARN2966 is a potent, orally active, and BBB penetrant post-transcriptional modulator of APP expression. It reduces APP expression and lowers Aβ production. It improves memory and reduces Aβ in Alzheimer's disease transgenic mice. This product is for research use only.
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| Molecular Formula |
C12H12N2O
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|---|---|
| Molecular Weight |
200.23648
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| Exact Mass |
200.095
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| CAS # |
102212-26-0
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| PubChem CID |
14936865
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
2.472
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
15
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| Complexity |
187
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
GXJRVWZNMZGWAQ-UHFFFAOYSA-N
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| InChi Code |
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
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| Chemical Name |
2-(pyridin-2-ylmethylamino)phenol
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| Synonyms |
ARN-2966; ARN 2966; ARN2966; 2-PMAP; 2 PMAP
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~110 mg/mL (~549.34 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.75 mg/mL (13.73 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 27.5 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.75 mg/mL (13.73 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 27.5 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.9940 mL | 24.9700 mL | 49.9401 mL | |
| 5 mM | 0.9988 mL | 4.9940 mL | 9.9880 mL | |
| 10 mM | 0.4994 mL | 2.4970 mL | 4.9940 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Products are for research use only; We do not sell to patients
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