Size | Price | Stock | Qty |
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50mg |
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100mg |
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250mg |
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500mg |
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1g |
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2g |
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5g |
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Purity: ≥98%
Cytisine (Baphitoxine,Sophorine; Citizin; HSDB-3560; Laburnin; NSC-407282; Cytisinicline), a nicotinic acetylcholine receptor agonist, is a naturally occuring alkaloid found in several plant genera, such as Laburnum and Cytisus of the family Fabaceae. It has been used medically to help with smoking cessation. It is a potent agonist selective for neuronal nAChRs (Ki = 2, 5890, 480, 329, and 492 nM at α4β2, α7, α3β4, α6/α4β4, α1β1γδ, respectively).
ln Vitro |
In HepG2 cells, cytosinicline (Cytisine) at 2.5, 5 and 10 mM can cause apoptosis [4]. Phase G1 (P<0.01). The population of sub-G1 cells is greatly increased when HepG2 cells are preincubated with Cytisinicline (Cytisine) at concentrations of 2.5, 5, and 10 mM [4].
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ln Vivo |
Compared to those receiving vehicle, individuals on cytisinicline (5 mg/kg, ip) ate less and gained less weight [2]. Animals self-administered Cytisine substantially less than nicotine, and total particle intake rose with Cytisinicline (Cytisine) substitution compared with nicotine [2].
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Animal Protocol |
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References |
[1]. Pabreza LA, et al. [3H]cytisine binding to nicotinic cholinergic receptors in brain. Mol Pharmacol. 1991 Jan;39(1):9-12.
[2]. Grebenstein PE, et al. The effects of noncontingent and self-administered cytisine on body weight and meal patterns in male Sprague-Dawley rats. Pharmacol Biochem Behav. 2013 Sep;110:192-200. [3]. Walker N, et al. Cytisine versus nicotine for smoking cessation. N Engl J Med. 2014 Dec 18;371(25):2353-62. [4]. Yu L, et al. Cytisine induces endoplasmic reticulum stress caused by calcium overload in HepG2 cells. Oncol Rep. 2018 Mar;39(3):1475-1484. |
Molecular Formula |
C11H14N2O
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Molecular Weight |
190.24
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CAS # |
485-35-8
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
O=C1C([H])=C([H])C([H])=C2[C@@]3([H])C([H])([H])N([H])C([H])([H])[C@@]([H])(C([H])([H])N21)C3([H])[H]
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InChi Key |
ANJTVLIZGCUXLD-DTWKUNHWSA-N
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InChi Code |
InChI=1S/C11H14N2O/c14-11-3-1-2-10-9-4-8(5-12-6-9)7-13(10)11/h1-3,8-9,12H,4-7H2/t8-,9+/m0/s1
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Chemical Name |
(1R,5S)-1,2,3,4,5,6-hexahydro-8H-1,5-methanopyrido[1,2-a][1,5]diazocin-8-one
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Synonyms |
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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 |
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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) |
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (10.93 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 20.8 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: ≥ 2.08 mg/mL (10.93 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 20.8 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: ≥ 2.08 mg/mL (10.93 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 | 5.2565 mL | 26.2826 mL | 52.5652 mL | |
5 mM | 1.0513 mL | 5.2565 mL | 10.5130 mL | |
10 mM | 0.5257 mL | 2.6283 mL | 5.2565 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.
NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
NCT03268343 | Completed Has Results | Drug: Cytisine | Smoking Cessation | Achieve Life Sciences | August 8, 2017 | Phase 1 |
NCT05729243 | Recruiting | Drug: Cytisine Other: Placebo |
Tobacco Use Disorder Alcohol Use Disorder Smoking Cessation |
Centre for Addiction and Mental Health | February 8, 2023 | Phase 4 |
NCT04015414 | Completed | Drug: Varenicline Drug: Cytisine |
Smoking Cessation | University of Zagreb | July 14, 2020 | Phase 3 |
NCT06439303 | Recruiting | Drug: Cytisine 1,5 mg | Moderate or Severe Tobacco Use Disorder |
Regina Elena Cancer Institute | March 20, 2024 | |
NCT02585024 | Terminated | Drug: Cytisine | Smoking Cessation | University of Auckland, New Zealand | February 2016 | Phase 1 |
Changes in body weight over treatment and cessation phases for vehicle and cytisine treated groups in Experiment 1. Shown are mean +/− SE cumulative change in body weight (g) on consecutive days of treatment and cessation phases, in rats that received either cytisine (n = 8) or vehicle (n = 8). *P < 0.1, **P < 0.01 difference between vehicle and cytisine.[1]. The effects of noncontingent and self-administered cytisine on body weight and meal patterns in male Sprague-Dawley rats. Pharmacol Biochem Behav. 2013 Sep;110:192-200. td> |
Total number of pellets consumed in the various phases of Experiment 1. Shown are mean +/− SE lever presses for pellets consumed, averaged over the ranges of days indicated during 23 hours (a), the dark period (b), or the light period (c), in rats that received either vehicle (n = 8) or cytisine (n = 8) during the treatment phase. *P < 0.05, **P < 0.01 difference between vehicle and cytisine.[1]. The effects of noncontingent and self-administered cytisine on body weight and meal patterns in male Sprague-Dawley rats. Pharmacol Biochem Behav. 2013 Sep;110:192-200. td> |
Total meal number during the various phases of Experiment 1. Shown are mean +/− SE number of meals, averaged over the ranges of days indicated during 23 hours (a), the dark period (b), or the light period (c), in rats that received either vehicle (n = 8) or cytisine (n = 8) during the treatment phase. *P < 0.05, **P < 0.01 difference between vehicle and cytisine.[1]. The effects of noncontingent and self-administered cytisine on body weight and meal patterns in male Sprague-Dawley rats. Pharmacol Biochem Behav. 2013 Sep;110:192-200. td> |