| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
alpha4beta2 neuronal nicotinic acetylcholine receptor. High affinity (Ki in sub‑nanomolar range for the active enantiomer; racemate shows somewhat lower affinity). Selectivity over alpha7 and alpha3beta4 nAChRs is >100‑fold. Also binds to alpha4alpha6beta2beta3 subtypes with moderate affinity.
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| 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].
Full agonist at alpha4beta2 nAChRs in vitro, stimulating rubidium efflux with EC50 in the low nanomolar range (around 5‑15 nM for the active enantiomer). In synaptosomes, it increases dopamine and norepinephrine release, which is believed to contribute to antidepressant‑like effects. No significant activity at alpha7 or muscle nAChRs. |
| ln Vivo |
In vivo, (Rac)‑CP‑601927 produces antidepressant‑like effects in the forced swim test and tail suspension test in mice (ED50 ~0.1‑0.3 mg/kg i.p.). It reduces anxiety‑like behavior in the elevated plus maze. Effects are blocked by the nAChR antagonist mecamylamine. It also attenuates nicotine self‑administration in rats, suggesting potential for smoking cessation.
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| Enzyme Assay |
Use rat cerebral cortical membranes (200 microg protein) expressing alpha4beta2 nAChRs. Incubate with 0.5 nM [3H]‑cytisine and (Rac)‑CP‑601927 (0.001 nM‑10 microM) in 50 mM Tris‑HCl pH 7.4 containing 120 mM NaCl, 5 mM KCl, 2 mM CaCl2, 1 mM MgCl2 for 60 min at 22degC. Non‑specific: 10 microM (−)‑nicotine. Filter through GF/B (0.5% PEI), wash 3×, count by scintillation. Determine IC50 and calculate Ki.
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| Cell Assay |
Use K177 cells stably expressing human alpha4beta2 nAChR. Seed in 96‑well plates (50,000/well) in DMEM/10% FBS/Geneticin for 48 h. Load with 1 microCi/well ⁸⁶Rb+ for 90 min at 37degC. Wash 3×, add (Rac)‑CP‑601927 (0.01 nM‑10 microM) for 5 min. Transfer supernatant to scintillation plates. Lyse cells with 1% SDS and count lysate. Calculate % efflux = (supernatant cpm)/(supernatant + lysate cpm) × 100. Fit to obtain EC50.
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| Animal Protocol |
Male CD‑1 mice (20‑30 g) for forced swim test. Administer (Rac)‑CP‑601927 (0.03‑1 mg/kg i.p.) 30 min before test. Place mouse in a cylinder of water (25degC, 6 cm diameter, 10 cm depth) for 6 min. Measure immobility time during the last 4 min. Reduced immobility vs. vehicle indicates antidepressant‑like effect. Control with mecamylamine (1 mg/kg i.p.) given 15 min before test to block effect. Also test in elevated plus maze (5 min) for anxiety: measure time in open arms.
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| ADME/Pharmacokinetics |
Oral bioavailability estimated ~40‑60% in rats. Brain‑to‑plasma ratio ~0.8‑1.2. t½ ~2‑3 h in rodents. Primary metabolic route: oxidation of the pyridine ring and N‑dealkylation by CYP2D6 and CYP3A4. Excretion mainly in urine. Linear PK at 0.1‑3 mg/kg.
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| Toxicity/Toxicokinetics |
Well tolerated at efficacious doses (0.03‑1 mg/kg) with no overt toxicity. At high doses (>10 mg/kg), mild tremor and decreased locomotor activity observed. No significant effects on blood pressure or heart rate in anesthetized rats. No mutagenicity in standard assays. Long‑term safety data not available as it is a research compound.
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| References | |
| Additional Infomation |
alpha4beta2 nAChR agonist. Antidepressant and anxiolytic effects likely via increased release of dopamine and norepinephrine in prefrontal cortex and nucleus accumbens. Was under preclinical development but not advanced to clinical trials. Not FDA‑approved. CAS 230615‑01‑7. Used only for laboratory research on nAChR pharmacology, mood disorders, and addiction.
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| Molecular Formula |
C12H13CLF3N
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|---|---|
| Molecular Weight |
263.69
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| Exact Mass |
263.068
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| CAS # |
230615-01-7
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| Related CAS # |
CP-601927;357425-02-6;CP-601932;357425-68-4
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| PubChem CID |
9881717
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| Appearance |
Off-white to light yellow solid powder
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
0
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| Heavy Atom Count |
17
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| Complexity |
276
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1C2C3C(=CC(=CC=3)C(F)(F)F)C1CNC2.Cl
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| InChi Key |
ZHTWFWUVFSXTNF-UHFFFAOYSA-N
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| 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
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| Chemical Name |
4-(trifluoromethyl)-10-azatricyclo[6.3.1.02,7]dodeca-2(7),3,5-triene;hydrochloride
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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 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)
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| Solubility (In Vitro) |
DMSO: 100 mg/mL (379.23 mM)
H2O: 100 mg/mL (379.23 mM) |
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| 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. View More
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. |
| 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.
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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