GLPBio

N-Nornuciferine

Catalog No.: GC36754Purity:>98.00%Synonyms: Daechualkaloid E, (R)-Nornuciferine, (-)-Nornuciferine, Sanjoinine Ia
COASDSData Sheet
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.

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N-Nornuciferine
Cas No.: 4846-19-9
5mgIn Stock
$213.00
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10mgIn Stock
$367.00
1
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Description

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.

Protocol

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].

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.

Product Documents

Purity:>98.00%Appearance:A solid
COASDSData Sheet

Chemical Properties

CAS No.
4846-19-9
Synonyms
Daechualkaloid E, (R)-Nornuciferine, (-)-Nornuciferine, Sanjoinine Ia
SMILES
COC1=C(OC)C2=C3C(CCN[C@]3([H])CC4=CC=CC=C24)=C1
Molecular Formula
C18H19NO2
Molecular Weight
281.35
Solubility
DMSO : 100 mg/mL (355.43 mM; Need ultrasonic)
Storage
Store at -20°C,protect from light
General tips
Select a suitable solvent according to the product solubility data. Once prepared, aliquot the stock solution to avoid repeated freeze-thaw cycles.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Shipping Condition
Evaluation samples are shipped with blue ice. Other available sizes are shipped at room temperature or with blue ice upon request.

CalculatorsMolarity / Dilution / Molecular Weight / Unit Conversion / In Vivo Formulation / Solubility

g/mol

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