| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| Targets |
CP-601927 targets the α4β2 nicotinic acetylcholine receptor (nAChR). It acts as a selective partial agonist with a Ki of 1.2 nM and an EC50 of 2.6 µM. The compound exhibits high affinity for the α4β2 subtype and good brain penetration. By partially activating α4β2 nAChRs, CP-601927 modulates cholinergic neurotransmission, which is believed to underlie its antidepressant-like properties.
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| ln Vitro |
In vitro, CP-601927 acts as a selective α4β2 nAChR partial agonist with a Ki of 1.2 nM and an EC50 of 2.6 µM. Its high affinity for the α4β2 receptor subtype makes it a valuable tool for studying nAChR pharmacology. The compound's activity is typically assessed in receptor binding assays and functional assays measuring ion flux or downstream signaling in cells expressing α4β2 nAChRs.
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| 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].
In vivo, CP-601927 demonstrates antidepressant-like activity in animal models. It is administered via intraperitoneal injection at doses ranging from 0.125 to 1.5 mg/kg. The compound's good brain penetration supports its central nervous system activity. Its antidepressant-like properties make it a candidate for studying the role of α4β2 nAChRs in depression. |
| Enzyme Assay |
In cell-free receptor binding assays, CP-601927's activity is evaluated by measuring its affinity for the α4β2 nAChR. Membrane preparations from cells expressing the receptor are incubated with a radiolabeled ligand (e.g., [3H]epibatidine) and varying concentrations of CP-601927. The displacement of the radioligand is measured, and the Ki (1.2 nM) is calculated from the competition curve.
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| Cell Assay |
In vitro cell-based experiments with CP-601927 typically involve cell lines expressing α4β2 nAChRs, such as HEK293 or CHO cells transfected with the receptor subunits. Cells are treated with the compound, and receptor activation is assessed by measuring ion flux (e.g., calcium influx using fluorescent dyes) or by electrophysiological techniques. The EC50 (2.6 µM) for receptor activation is determined from concentration-response curves.
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| Animal Protocol |
In vivo animal experiments with CP-601927 have been conducted to evaluate its antidepressant-like activity. In typical protocols, rodents are administered the compound via intraperitoneal injection at doses of 0.125-1.5 mg/kg. Behavioral tests such as the forced swim test or tail suspension test are performed to assess antidepressant-like effects. Brain penetration and receptor occupancy can also be measured.
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| ADME/Pharmacokinetics |
No detailed pharmacokinetic data is publicly available for CP-601927. The compound is described as CNS-penetrant with good brain penetration. It has a molecular formula of C12H12F3N and a molecular weight of 227.23. Its half-life and bioavailability have not been extensively characterized in the available literature.
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| Toxicity/Toxicokinetics |
No specific toxicity data is publicly available for CP-601927. In preclinical studies, the compound has shown antidepressant-like activity without reported significant toxicity. The compound is for research use only and is not intended for human therapeutic applications.
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| References |
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| Additional Infomation |
CP-601,927 has been used in trials investigating the basic science and treatment of major depressive disorder.
CP-601927 has a molecular formula of C12H12F3N and a molecular weight of 227.23. It is a CNS-penetrant, high affinity, and selective α4β2 nAChR partial agonist with a Ki of 1.2 nM and an EC50 of 2.6 µM. The compound shows good brain penetration and antidepressant-like properties. It is available for research purposes only. |
| Molecular Formula |
C12H12F3N
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|---|---|
| Molecular Weight |
227.225593566895
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| Exact Mass |
227.092
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| CAS # |
357425-02-6
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| Related CAS # |
(Rac)-CP-601927 hydrochloride;230615-01-7;CP-601932;357425-68-4
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| PubChem CID |
11498153
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| Appearance |
Light yellow to brown liquid
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| LogP |
2.4
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
0
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| Heavy Atom Count |
16
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| Complexity |
276
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| Defined Atom Stereocenter Count |
2
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| SMILES |
C1[C@H]2CNC[C@@H]1C3=C2C=CC(=C3)C(F)(F)F
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| InChi Key |
RNOBTWYQAWEZHH-JGVFFNPUSA-N
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| 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
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| Chemical Name |
(1S,8R)-4-(trifluoromethyl)-10-azatricyclo[6.3.1.02,7]dodeca-2(7),3,5-triene
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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 : ~200 mg/mL (~880.17 mM)
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| 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.
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.
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