ARN2966 is a novel and potent post-transcriptional modulator of APP (amyloid precursor protein) expression; reduces expression of APP with resultant lower production of Aβ. The mechanism of action (MOA) of ARN2966 is currently under study and appears to be novel. ARN2966 reduces expression of APP with resultant lower production of 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.

Physicochemical Properties

Molecular Formula	C12H12N2O
Molecular Weight	200.23648
Exact Mass	200.095
CAS #	102212-26-0
PubChem CID	14936865
Appearance	Light yellow to yellow solid powder
LogP	2.472
Hydrogen Bond Donor Count	2
Hydrogen Bond Acceptor Count	3
Rotatable Bond Count	3
Heavy Atom Count	15
Complexity	187
Defined Atom Stereocenter Count	0
InChi Key	GXJRVWZNMZGWAQ-UHFFFAOYSA-N
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
Chemical Name	2-(pyridin-2-ylmethylamino)phenol
Synonyms	ARN-2966; ARN 2966; ARN2966; 2-PMAP; 2 PMAP
HS Tariff Code	2934.99.9001
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)

Biological Activity

References

:http://arianeurosciences.com/science.html

Solubility Data

Solubility (In Vitro)

DMSO : ~110 mg/mL (~549.34 mM)

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.