N-Nornuciferine
Based on 1 publication(s) in Google Scholar
N-Nornuciferine is an orally active, blood-brain barrier-permeable CYP2D6 inhibitor, with an IC50 of 3.76 μM and a Ki of 2.34 μM against human CYP2D6. N-Nornuciferine also acts as a BChE inhibitor, showing an IC50 of 5.6 μM in mice. N-Nornuciferine can be used in the research of neurological-related diseases.
For research use only. We do not sell to patients.
- Purity: 99.92%
- CAS No.: 4846-19-9
- Formula: C18H19NO2
- Molecular Weight:281.35
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocol
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) N-Nornuciferine
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Biological Activity
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CYP2D6 3.76 μM (IC50) |
CYP2D6 2.34 μM (Ki) |
BChE 5.6 μM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| B16-4A5 | IC50 |
62.9 μM
Compound: 4
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Inhibition of melanogenesis in mouse B16-4A5 cells after 72 hrs by spectrophotometry
Inhibition of melanogenesis in mouse B16-4A5 cells after 72 hrs by spectrophotometry
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[PMID: 23270663] |
N-nornuciferine potently inhibits CYP2D6 in pooled human liver microsomes via competitive inhibition (IC50 = 3.76 μM, Ki = 2.34 μM), while it only exerts weak inhibitory effects on CYP2C19 (IC50 = 29 μM)[1].
N-Nornuciferine (Compound 5) is a BChE inhibitor with an IC50 of 5.6 μM in mice[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| Species | Dose | Route | Tmax | Cmax | T1/2 | AUC0-t | AUC0-inf | Vz | MRTINF_obs | Bioavailability | CL | C0 | Vd/F | CL/F |
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Rat[2] | 10 mg/kg | p.o. | 1.65 h | 0.57 μg/mL | 2.94 h | 3.32 μg·h/mL | 3.40 μg·h/mL | 10.34 L/kg | 4.71 h | 79.91 % | 2.44 L/h/kg | / | / | / |
| Rat[2] | 2 mg/kg | i.v. | 0.00 h | / | 3.84 h | 0.74 μg·h/mL | 0.85 μg·h/mL | 15.17 L/kg | 4.94 h | / | 2.61 L/h/kg | 0.69 μg/mL | / | / |
| Rat[2] | 4 mg/kg | i.v. | 1.22 h | 0.16 h | 1.39 h | 0.46 μg·h/mL | 0.5 μg·h/mL | / | 2.98 h | / | / | / | 16.17 L/kg | 8.08 L/h/kg |
Chemical Information
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CAS No. 4846-19-9
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Appearance Solid
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Molecular Weight 281.35
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Formula C18H19NO2
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Color Off-white to light yellow
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SMILES
COC1=C(OC)C2=C3C(CCN[C@]3([H])CC4=CC=CC=C24)=C1
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Structure Classification
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Initial Source
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
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Carbohydr Polym
Metabolic degradation of lentinan in liver mediated by CYP450 enzymes and epoxide hydrolase. [Abstract]2021 Feb 1;253:117255. PMID: 33279005
Solvent & Solubility
DMSO : 100 mg/mL (355.43 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (8.89 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (8.89 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
For the determination of the inhibition constant Ki values, various final concentrations of the specific substrate dextromethorphan for CYP2D6 in the range of 1 to 10 mM and different concentrations of the N-Nornuciferine in the range of 0 to 25 mM are used. After preincubation for 10 min, the reactions are initiated by the addition of NADPH. Each incubation test is performed in triplicate. Thirty minutes after the incubation is initiated, the reaction is stopped by the addition of 100 mL of ice-cold acetonitrile containing 1 mg/mL propranolol (IS). The incubation mixtures are then centrifuged at 15,000g for 10 min at 4 °C. Ten-microliter aliquots of the supernatants are injected into an LC-MS/MS system[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (281 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Ye LH, et al. Identification and characterization of potent CYP2D6 inhibitors in lotus leaves. J Ethnopharmacol. 2014 Apr 11;153(1):190-6. [Content Brief]
[2]. Ye LH, et al. Pharmacokinetics of Nuciferine and N-Nornuciferine, Two Major Alkaloids From Nelumbo nucifera Leaves, in Rat Plasma and the Brain. Front Pharmacol. 2018 Aug 29;9:902. [Content Brief]
[3]. Cometa MF, et al. New cholinesterase inhibiting bisbenzylisoquinoline alkaloids from Abuta grandifolia. Fitoterapia. 2012 Apr;83(3):476-80. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.5543 mL | 17.7715 mL | 35.5429 mL | 88.8573 mL |
| 5 mM | 0.7109 mL | 3.5543 mL | 7.1086 mL | 17.7715 mL | |
| 10 mM | 0.3554 mL | 1.7771 mL | 3.5543 mL | 8.8857 mL | |
| 15 mM | 0.2370 mL | 1.1848 mL | 2.3695 mL | 5.9238 mL | |
| 20 mM | 0.1777 mL | 0.8886 mL | 1.7771 mL | 4.4429 mL | |
| 25 mM | 0.1422 mL | 0.7109 mL | 1.4217 mL | 3.5543 mL | |
| 30 mM | 0.1185 mL | 0.5924 mL | 1.1848 mL | 2.9619 mL | |
| 40 mM | 0.0889 mL | 0.4443 mL | 0.8886 mL | 2.2214 mL | |
| 50 mM | 0.0711 mL | 0.3554 mL | 0.7109 mL | 1.7771 mL | |
| 60 mM | 0.0592 mL | 0.2962 mL | 0.5924 mL | 1.4810 mL | |
| 80 mM | 0.0444 mL | 0.2221 mL | 0.4443 mL | 1.1107 mL | |
| 100 mM | 0.0355 mL | 0.1777 mL | 0.3554 mL | 0.8886 mL |
N-Nornuciferine Related Classifications
HY-N2129 Related Classifications
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