| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| Other Sizes |
| Targets |
- N-Methylcytisine is a selective ligand for central nervous system (CNS) nicotinic acetylcholine receptors (nAChRs). [2]
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|---|---|
| ln Vivo |
- Amelioration of DSS-Induced Colitis in Mice: Male C57BL/6 mice (6–8 weeks old) were given 3.5% dextran sulfate sodium (DSS) in drinking water for 7 days to induce acute colitis. N-Methylcytisine was administered via intraperitoneal injection at doses of 10 mg/kg or 20 mg/kg once daily for 7 days, with the following results:
1. Body weight loss was reduced: from ~25% (DSS control) to ~10% (10 mg/kg) and ~15% (20 mg/kg); 2. Colon length was increased: from ~4.5 cm (DSS control) to ~6.0 cm (10 mg/kg) and ~6.5 cm (20 mg/kg); 3. Histological damage scores (based on epithelial erosion and inflammatory infiltration) decreased: from ~8 (DSS control) to ~5 (10 mg/kg) and ~3 (20 mg/kg); 4. Colonic pro-inflammatory cytokines (TNF-α, IL-6, IL-1β) levels decreased by ~40%–60% (ELISA detection), and NF-κB p65 phosphorylation was downregulated (western blot detection). [1] |
| Enzyme Assay |
- CNS nAChR Binding Assay: Crude membrane fractions were isolated from rat CNS tissues (cerebral cortex and hippocampus). The assay mixture contained membrane fractions, [³H]-nicotine (radiolabeled nAChR ligand), and N-Methylcytisine (0–100 μM). After incubation at 25°C for 60 minutes, the mixture was filtered through glass fiber filters to separate bound and free ligands. Radioactivity of the filters was measured via liquid scintillation counting to assess the displacement of [³H]-nicotine by N-Methylcytisine, confirming its selective binding to CNS nAChRs. [2]
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| Animal Protocol |
- DSS-Induced Colitis Mouse Model:
1. Male C57BL/6 mice (6–8 weeks old, 20–22 g) were acclimated for 1 week with free access to food and water; 2. Mice drank 3.5% DSS (molecular weight 36,000–50,000) for 7 consecutive days to induce colitis; 3. N-Methylcytisine was dissolved in normal saline, and administered via intraperitoneal injection at 10 mg/kg or 20 mg/kg once daily for 7 days; the control group received equal volumes of normal saline; 4. On day 8, mice were euthanized. Colons were harvested to measure length, and colonic tissues were collected for histological analysis, ELISA, and western blot. [1] |
| References |
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| Additional Infomation |
N-methylcytosine has been reported to be present in Maackia tenuifolia, Thermopsis lanceolata, and other organisms with relevant data.
See also: Methylcytosine (note moved here). - N-methylcytosine alleviates DSS-induced colitis by inhibiting the NF-κB signaling pathway and reducing the production of pro-inflammatory cytokines, thereby protecting the intestinal epithelial barrier and reducing inflammatory cell infiltration. [1] - N-methylcytosine preferentially binds to central nervous system nAChRs rather than peripheral nAChRs. [2] |
| Molecular Formula |
C12H16N2O
|
|---|---|
| Molecular Weight |
204.2682
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| Exact Mass |
204.126
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| Elemental Analysis |
C, 69.45; H, 7.42; N, 14.73; O, 8.41
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| CAS # |
486-86-2
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| PubChem CID |
670971
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| Appearance |
White to off-white solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
400.8±34.0 °C at 760 mmHg
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| Melting Point |
137-139ºC
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| Flash Point |
191.9±18.0 °C
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| Vapour Pressure |
0.0±0.9 mmHg at 25°C
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| Index of Refraction |
1.616
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| LogP |
0.46
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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 |
15
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| Complexity |
359
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| Defined Atom Stereocenter Count |
2
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| SMILES |
O=C1C([H])=C([H])C([H])=C2C3([H])C([H])([H])N(C([H])([H])[H])C([H])([H])[C@@]([H])(C([H])([H])N21)C3([H])[H]
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| InChi Key |
CULUKMPMGVXCEI-VHSXEESVSA-N
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| InChi Code |
InChI=1S/C12H16N2O/c1-13-6-9-5-10(8-13)11-3-2-4-12(15)14(11)7-9/h2-4,9-10H,5-8H2,1H3/t9-,10+/m0/s1
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| Chemical Name |
(1R,9S)-11-methyl-7,11-diazatricyclo[7.3.1.02,7]trideca-2,4-dien-6-one
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| Synonyms |
BRN0012448; BRN-0012448; BRN 0012448; Caulophylline
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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: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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 : ~120 mg/mL (~587.46 mM)
H2O : ~100 mg/mL (~489.55 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (10.18 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 (10.18 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 (10.18 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 | 4.8955 mL | 24.4774 mL | 48.9548 mL | |
| 5 mM | 0.9791 mL | 4.8955 mL | 9.7910 mL | |
| 10 mM | 0.4895 mL | 2.4477 mL | 4.8955 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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