| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg | |||
| Other Sizes |
| Targets |
N-Formylcytisine targets nicotinic acetylcholine receptors (nAChRs), specifically the α4β2 subtype, with high affinity. It acts as a partial agonist at these receptors, meaning it activates the receptor but with lower efficacy than a full agonist. This mechanism makes it a valuable pharmacological tool for studying receptor desensitization, neurotransmitter release, and the neurobiological pathways underlying addiction. The compound's structural similarity to nicotine explains its affinity for nAChRs and its potential applications in addiction research.
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| ln Vitro |
In vitro, N-Formylcytisine binds with high affinity to the α4β2 nAChR subtype. It is used in in vitro binding assays to study nicotinic acetylcholine receptors in neuropharmacology. As a partial agonist, it modulates receptor activity and can be used to investigate receptor desensitization and neurotransmitter release mechanisms. The compound's structural similarity to nicotine makes it a candidate for research in neuropharmacology and cancer treatment. Specific binding affinities or IC50 values are not detailed in the available literature.
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| ln Vivo |
Specific in vivo data for N-Formylcytisine are limited in the available literature. The compound is used in in vivo behavioral models to study nicotinic receptor function and addiction pathways. Given its structural similarity to cytisine, which has been studied as a smoking cessation aid, N-Formylcytisine may have potential for in vivo studies in addiction models. Its role as a partial agonist at α4β2 nAChRs suggests potential for modulating dopamine release and reward pathways. However, specific published in vivo protocols are not available.
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| Enzyme Assay |
The nicotinic acetylcholine receptor binding affinity is assessed using radioligand binding assays. Membrane preparations from cells expressing recombinant α4β2 nAChRs are incubated with a radiolabeled ligand (e.g., [³H]epibatidine or [³H]cytisine) and various concentrations of N-Formylcytisine. Specific binding is determined, and Ki or IC50 values are calculated from competition binding curves. Functional activity (agonist or partial agonist) is assessed using calcium flux assays or electrophysiological recordings in cells expressing nAChRs.
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| Cell Assay |
For cellular studies, cell lines expressing nAChR subtypes (e.g., HEK293 cells transfected with α4β2 subunits) are cultured in appropriate media. Cells are treated with N-Formylcytisine at various concentrations, and receptor activation is measured using calcium-sensitive fluorescent dyes (e.g., Fluo-4) or by patch-clamp electrophysiology. For binding assays, membrane preparations are used. Cell viability may be assessed using standard assays for cytotoxicity evaluation.
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| Animal Protocol |
In vivo behavioral studies for nicotinic receptor ligands are conducted in rodent models. Compounds are administered via intraperitoneal injection or oral gavage, and behavioral effects are assessed using tests such as conditioned place preference (for reward/addiction studies), locomotor activity, and anxiety-related tests. For addiction research, self-administration models or nicotine withdrawal models may be used. However, specific published protocols for N-Formylcytisine are not available.
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| ADME/Pharmacokinetics |
Specific pharmacokinetic data for N-Formylcytisine are not reported. As a cytisine alkaloid with molecular weight 218.25 g/mol, the compound is expected to have moderate lipophilicity and potential for oral absorption and blood-brain barrier penetration. Cytisine itself is known to be orally bioavailable and to cross the blood-brain barrier. Pharmacokinetic studies would be required to determine parameters such as half-life, Cmax, and bioavailability for N-Formylcytisine. The compound is soluble in chloroform, ethanol, and methanol.
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| Toxicity/Toxicokinetics |
Toxicological data for N-Formylcytisine are limited. As a nicotinic receptor ligand, the compound may have dose-dependent effects on the nervous system, including potential for seizures, respiratory depression, or cardiovascular effects at high doses. Cytisine and related alkaloids have been studied for their safety profiles in smoking cessation research. Comprehensive toxicology studies would be required before any therapeutic development. The compound should be handled with appropriate safety precautions.
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| References | |
| Additional Infomation |
(-)-N-formyl cytisine has been reported in Maackia tenuifolia, Thermopsis lanceolata, and other organisms with available data.
N-Formylcytisine is a cytisine-type alkaloid from Maackia amurensis that acts as a high-affinity partial agonist at α4β2 nAChRs. It is used in neuropharmacology research on receptor desensitization, neurotransmitter release, and addiction pathways. No clinical trials or approvals exist. For research use only. |
| Molecular Formula |
C12H14N2O2
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|---|---|
| Molecular Weight |
218.2518
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| Exact Mass |
218.106
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| CAS # |
53007-06-0
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| PubChem CID |
179619
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| Appearance |
White to off-white solid
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| Density |
1.31±0.1 g/cm3(Predicted)
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| Boiling Point |
512.8±49.0 °C(Predicted)
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| LogP |
0.997
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
0
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| Heavy Atom Count |
16
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| Complexity |
400
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| Defined Atom Stereocenter Count |
2
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| SMILES |
O=C1C([H])=C([H])C([H])=C2[C@@]3([H])C([H])([H])N(C([H])=O)C([H])([H])[C@@]([H])(C([H])([H])N21)C3([H])[H]
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| InChi Key |
PCYQRXYBKKZUSR-VHSXEESVSA-N
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| InChi Code |
InChI=1S/C12H14N2O2/c15-8-13-5-9-4-10(7-13)11-2-1-3-12(16)14(11)6-9/h1-3,8-10H,4-7H2/t9-,10+/m0/s1
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| Chemical Name |
(1R,9S)-6-oxo-7,11-diazatricyclo[7.3.1.02,7]trideca-2,4-diene-11-carbaldehyde
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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 : ~100 mg/mL (~458.19 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (11.45 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 (11.45 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 (11.45 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 | 4.5819 mL | 22.9095 mL | 45.8190 mL | |
| 5 mM | 0.9164 mL | 4.5819 mL | 9.1638 mL | |
| 10 mM | 0.4582 mL | 2.2910 mL | 4.5819 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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