N-Nornuciferine (Synonyms: Daechualkaloid E, (R)-Nornuciferine, (-)-Nornuciferine, Sanjoinine Ia) |
| カタログ番号GC36754 |
N-ノルヌシフェリンはハスの葉に含まれるアポルフィン アルカロイドで、CYP2D6 を有意に阻害します。IC50 と Ki はそれぞれ 3.76 μM と 2.34 μM です。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 4846-19-9
Sample solution is provided at 25 µL, 10mM.
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N-Nornuciferine is an aporphine alkaloid in lotus leaf that significantly inhibits CYP2D6 with IC50 and Ki of 3.76 and 2.34 μM, respectively. IC50: 3.76 μM (CYP2D6)[1]Ki: 2.34 μM (CYP2D6)[1]
The herb of lotus leaves is a commonly used traditional Chinese medicine with a wide range of pharmacological and physiological activities, particularly the reduction of the blood triglyceride and cholesterol levels. N-Nornuciferine strongly inhibits CYP2D6 activity but shows weak or no inhibition of the other four P450 isoenzymes (CYP2C19, CYP3A4, CYP2E1, CYP2C9). N-Nornuciferine competitively inhibits the CYP2D6-catalyzed dextromethorphan o-demethylation with apparent Ki values of 2.34 μM[1].
[1]. Ye LH, et al. Identification and characterization of potent CYP2D6 inhibitors in lotus leaves. J Ethnopharmacol. 2014 Apr 11;153(1):190-6.
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Kinase experiment: |
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]. |
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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. |
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| Cas No. | 4846-19-9 | SDF | |
| 同義語 | Daechualkaloid E, (R)-Nornuciferine, (-)-Nornuciferine, Sanjoinine Ia | ||
| Canonical SMILES | COC1=C(OC)C2=C3C(CCN[C@]3([H])CC4=CC=CC=C24)=C1 | ||
| Formula | C18H19NO2 | M.Wt | 281.35 |
| 溶解度 | DMSO : 100 mg/mL (355.43 mM; Need ultrasonic) | Storage | Store at -20°C,protect from light |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.5543 mL | 17.7715 mL | 35.5429 mL |
| 5 mM | 0.7109 mL | 3.5543 mL | 7.1086 mL |
| 10 mM | 0.3554 mL | 1.7771 mL | 3.5543 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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