(Rac)-CP-601927 HCl is the racemate of CP-601927. CP-601927 is a nAChR agonist/activator with Kis of 1.2 nM and 102 nM for α4β2 and α3β4 nAChR, respectively.

Physicochemical Properties

Molecular Formula	C12H13CLF3N
Molecular Weight	263.69
Exact Mass	263.068
CAS #	230615-01-7
Related CAS #	CP-601927;357425-02-6;CP-601932;357425-68-4
PubChem CID	9881717
Appearance	Off-white to light yellow solid powder
Hydrogen Bond Donor Count	2
Hydrogen Bond Acceptor Count	4
Rotatable Bond Count	0
Heavy Atom Count	17
Complexity	276
Defined Atom Stereocenter Count	0
SMILES	C1C2C3C(=CC(=CC=3)C(F)(F)F)C1CNC2.Cl
InChi Key	ZHTWFWUVFSXTNF-UHFFFAOYSA-N
InChi Code	InChI=1S/C12H12F3N.ClH/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;1H
Chemical Name	4-(trifluoromethyl)-10-azatricyclo[6.3.1.02,7]dodeca-2(7),3,5-triene;hydrochloride
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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture.
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 mice, CP-601927 has strong antidepressant-like effects. CP-601927 may lessen cholinergic signaling by desensitization of α4β2* nAChRs or because of its decreased efficacy[1].
References	[1]. α4β2 nicotinic acetylcholine receptor partial agonists with low intrinsic efficacy have antidepressant-like properties. Behav Pharmacol. 2011 Aug;22(4):291-9.

Solubility Data

Solubility (In Vitro)

DMSO: 100 mg/mL (379.23 mM) H2O: 100 mg/mL (379.23 mM)

Solubility (In Vivo)

Solubility in Formulation 1: ≥ 2.5 mg/mL (9.48 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 25.0 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: ≥ 2.5 mg/mL (9.48 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 25.0 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: ≥ 2.5 mg/mL (9.48 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 25.0 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	3.7923 mL	18.9617 mL	37.9233 mL
	5 mM	0.7585 mL	3.7923 mL	7.5847 mL
	10 mM	0.3792 mL	1.8962 mL	3.7923 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.