FK962 is an enhancer of somatostatin release and has cognitive enhancement effects.

Physicochemical Properties

Molecular Formula	C₁₄H₁₇FN₂O₂
Molecular Weight	264.30
Exact Mass	264.127
CAS #	283167-06-6
Related CAS #	283167-06-6
PubChem CID	9816738
Appearance	White to off-white solid powder
Density	1.2±0.1 g/cm3
Boiling Point	474.4±40.0 °C at 760 mmHg
Flash Point	240.7±27.3 °C
Vapour Pressure	0.0±1.2 mmHg at 25°C
Index of Refraction	1.557
LogP	1.59
Hydrogen Bond Donor Count	1
Hydrogen Bond Acceptor Count	3
Rotatable Bond Count	2
Heavy Atom Count	19
Complexity	332
Defined Atom Stereocenter Count	0
InChi Key	VBHVOHJOTMCSBQ-UHFFFAOYSA-N
InChi Code	InChI=1S/C14H17FN2O2/c1-10(18)17-8-6-13(7-9-17)16-14(19)11-2-4-12(15)5-3-11/h2-5,13H,6-9H2,1H3,(H,16,19)
Chemical Name	N-(1-acetylpiperidin-4-yl)-4-fluorobenzamide
Synonyms	FK-962 FK962 FK962
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

ln Vitro	In rat hippocampus slices, FK962 (1 nM-1 μM) dramatically increases high K+-evoked somatostatin release. FK962 also dramatically decreased the somatostatin-induced Ca2+ channel inhibitory effect in individual rat hippocampus neurons at concentrations ranging from 1 to 100 nM using whole-cell patch clamp [1].
ln Vivo	Together, donepezil (single dose, 1 mg/kg) and FK962 (0.1, 0.3, or 1.0 mg/kg; i.p.) enhance cognitive function in rats and can be used as supplemental therapy for Alzheimer's disease [2].
Animal Protocol	Animal/Disease Models: Male Lister Hooded rat, weighing approximately 270-300 [2] Doses: 0.1, 0.3 or 1.0 mg/kg; donepezil administered as a single Doses: intraperitonealadministration Experimental Results: administered alone produces minimal cognitive enhancement. The effect of combination on cognition was Dramatically greater.
References	[1]. FK962, a novel enhancer of somatostatin release, exerts cognitive-enhancing actions in rats. Eur J Pharmacol. 2005 Dec 19;527(1-3):111-20. [2]. FK962 and donepezil act synergistically to improve cognition in rats: potential as an add-on therapy for Alzheimer's disease. Pharmacol Biochem Behav. 2011 Mar;98(1):76-80.

Solubility Data

Solubility (In Vitro)

DMSO : ~250 mg/mL (~945.89 mM) H2O : ~2 mg/mL (~7.57 mM)

Solubility (In Vivo)

Solubility in Formulation 1: ≥ 2.08 mg/mL (7.87 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 20.8 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: 2.08 mg/mL (7.87 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 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. Solubility in Formulation 3: ≥ 2.08 mg/mL (7.87 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.  (Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	3.7836 mL	18.9179 mL	37.8358 mL
	5 mM	0.7567 mL	3.7836 mL	7.5672 mL
	10 mM	0.3784 mL	1.8918 mL	3.7836 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.