| Size | Price | Stock | Qty |
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| Targets |
CP-601932 targets α4β2 nicotinic acetylcholine receptors (nAChRs). It acts as a selective partial agonist with high binding affinity for α4β2 and α3β4 nAChRs, and approximately 10-fold lower affinity for α6 and α7 isoforms. The compound is CNS-penetrant and is used as a research tool for studying nAChR pharmacology and neurological disorders.
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| ln Vitro |
In vitro, CP-601932 acts as a selective α4β2 nAChR partial agonist. It exhibits high binding affinity for α4β2 and α3β4 nAChRs, with an order of magnitude lower affinity for α6 and α7 isoforms. The compound's activity is typically assessed in receptor binding assays using radiolabeled ligands and in functional assays measuring ion flux in cells expressing nAChR subtypes.
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| ln Vivo |
CP-601932 (10 mg/kg; subcutaneous injection; adult male Sprague-Dawley rats) lowers active lever pressure for 10% ethanol but not for 5% sucrose in an operant self-administration paradigm [1] . CP-601932 (adult male Sprague-Dawley rats) easily penetrates the CNS and reaches maximum Cb,u values of 340 nM at 30 minutes after the 5 mg/kg dosage and 710 nM after the 10 mg/kg treatment. Brain concentrations of CP-601932 fall extremely slowly and levels remain reasonably high, such as 530 nM at 5 hours and 85 nM at 24 hours after 10 mg/kg [1].
No specific in vivo activity data is publicly available for CP-601932. As a CNS-penetrant α4β2 nAChR partial agonist, it is expected to have central nervous system effects similar to related compounds such as CP-601927. Further studies would be needed to establish its in vivo activity and potential therapeutic applications. |
| Enzyme Assay |
In cell-free receptor binding assays, CP-601932's activity is evaluated by measuring its affinity for α4β2 and other nAChR subtypes. Membrane preparations from cells expressing specific nAChR subtypes are incubated with radiolabeled ligands and varying concentrations of CP-601932. The displacement of the radioligands is measured, and the Ki values for each subtype are calculated from competition curves.
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| Cell Assay |
In vitro cell-based experiments with CP-601932 typically involve cell lines expressing specific nAChR subtypes, such as α4β2, α3β4, α6, or α7. Cells are treated with the compound, and receptor activation is assessed by measuring ion flux using fluorescent dyes or by electrophysiological techniques. The compound's selectivity profile is determined by comparing its potency at different nAChR subtypes.
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| Animal Protocol |
No specific in vivo animal protocols are publicly available for CP-601932. If in vivo studies were to be conducted, typical protocols might involve rodent models of neurological or psychiatric disorders, where the compound would be administered, and behavioral or physiological outcomes would be measured.
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| ADME/Pharmacokinetics |
No detailed pharmacokinetic data is publicly available for CP-601932. The compound is described as CNS-penetrant, indicating it can cross the blood-brain barrier. It has a molecular formula of C12H12F3N and a molecular weight of 227.23. Its half-life and bioavailability have not been extensively characterized.
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| Toxicity/Toxicokinetics |
No specific toxicity data is publicly available for CP-601932. As a research compound, its safety profile has not been well established. The compound is for research use only and is not intended for human therapeutic applications.
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| References | |
| Additional Infomation |
CP-601932 (free base) has a molecular formula of C12H12F3N and a molecular weight of 227.23. It is a selective α4β2 nAChR partial agonist. The compound has high binding affinity for α4β2 and α3β4 nAChRs, with approximately 10-fold lower affinity for α6 and α7 isoforms. It is CNS-penetrant and available for research purposes only.
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| Molecular Formula |
C12H12F3N
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|---|---|
| Molecular Weight |
227.225593566895
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| Exact Mass |
227.092
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| CAS # |
357425-68-4
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| Related CAS # |
CP-601927;357425-02-6;(Rac)-CP-601927 hydrochloride;230615-01-7
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| PubChem CID |
69604735
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| Appearance |
Light yellow to light brown ointment
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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-SFYZADRCSA-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+/m1/s1
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| Chemical Name |
(1R,8S)-4-(trifluoromethyl)-10-azatricyclo[6.3.1.02,7]dodeca-2(7),3,5-triene
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| Synonyms |
CP601932; CP 601932; CP-601932
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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% (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 50.0 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. (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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