CP-601927 is a selective α4β2 nAChR partial agonist (Ki=1.2 nM; EC50=2.6 μM). CP-601927 has good brain penetration and has antidepressant-like properties.

Physicochemical Properties

Molecular Formula	C12H12F3N
Molecular Weight	227.225593566895
Exact Mass	227.092
CAS #	357425-02-6
Related CAS #	(Rac)-CP-601927 hydrochloride;230615-01-7;CP-601932;357425-68-4
PubChem CID	11498153
Appearance	Light yellow to brown liquid
LogP	2.4
Hydrogen Bond Donor Count	1
Hydrogen Bond Acceptor Count	4
Rotatable Bond Count	0
Heavy Atom Count	16
Complexity	276
Defined Atom Stereocenter Count	2
SMILES	C1[C@H]2CNC[C@@H]1C3=C2C=CC(=C3)C(F)(F)F
InChi Key	RNOBTWYQAWEZHH-JGVFFNPUSA-N
InChi Code	InChI=1S/C12H12F3N/c13-12(14,15)9-1-2-10-7-3-8(6-16-5-7)11(10)4-9/h1-2,4,7-8,16H,3,5-6H2/t7-,8+/m0/s1
Chemical Name	(1S,8R)-4-(trifluoromethyl)-10-azatricyclo[6.3.1.02,7]dodeca-2(7),3,5-triene
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 Vivo	CP-601927 (0.125 mg/kg-1.5 mg/kg; i.p.; C57BL/6J male mice) shows antidepressant-like effects in animal models [2].
References	[1]. Toxicity study in juvenile rats with the α4β2 nicotinic acetylcholine receptor partial agonist CP-601,927. Birth Defects Res B Dev Reprod Toxicol. 2011;92(4):323-332. [2]. α4β2 nicotinic acetylcholine receptor partial agonists with low intrinsic efficacy have antidepressant-like properties. Behav Pharmacol. 2011;22(4):291-299.
Additional Infomation	CP-601,927 has been used in trials studying the basic science and treatment of Major Depressive Disorder.

Solubility Data

Solubility (In Vitro)

DMSO : ~200 mg/mL (~880.17 mM)

Solubility (In Vivo)

Solubility in Formulation 1: ≥ 5 mg/mL (22.00 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 50.0 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: ≥ 5 mg/mL (22.00 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 50.0 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	4.4008 mL	22.0041 mL	44.0083 mL
	5 mM	0.8802 mL	4.4008 mL	8.8017 mL
	10 mM	0.4401 mL	2.2004 mL	4.4008 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.