GLPBio

N-Nornuciferine

Catalog No.: GC36754Purity:>98.00%Synonyms: Daechualkaloid E, (R)-Nornuciferine, (-)-Nornuciferine, Sanjoinine Ia
COASDSData Sheet
La N-nornuciferina es un alcaloide de aporfina en la hoja de loto que inhibe significativamente CYP2D6 con IC50 y Ki de 3,76 y 2,34 μM, respectivamente.

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N-Nornuciferine
Cas No.: 4846-19-9
5mgIn Stock
$213.00
1
10mgIn Stock
$367.00
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    187(9):2288-2304 (2024)
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    183(7):1867-1883 (2020)
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Descripción (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.

Protocolo (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.

Documentos del producto (Product Documents)

Purity:>98.00%Appearance:A solid
COASDSData Sheet

Propiedades químicas (Chemical Properties)

N.º CAS
4846-19-9
Sinónimos
Daechualkaloid E, (R)-Nornuciferine, (-)-Nornuciferine, Sanjoinine Ia
SMILES
COC1=C(OC)C2=C3C(CCN[C@]3([H])CC4=CC=CC=C24)=C1
Fórmula molecular
C18H19NO2
Peso molecular
281.35
Solubilidad
DMSO : 100 mg/mL (355.43 mM; Need ultrasonic)
Almacenamiento
Store at -20°C,protect from light
Consejos generales
Seleccione un disolvente adecuado según los datos de solubilidad del producto. Una vez preparada, divida la solución madre en alícuotas para evitar ciclos repetidos de congelación y descongelación.
Utilice las soluciones madre en un plazo de 6 meses si se conservan a -80°C, o de 1 mes si se conservan a -20°C.
Para mejorar la solubilidad, caliente el tubo a 37°C y soníquelo durante un periodo adecuado.
Condiciones de envío
Las muestras de evaluación se envían con acumuladores de frío. Los demás tamaños se envían a temperatura ambiente o, previa solicitud, con acumuladores de frío.

Calculadoras (Calculators)Molaridad / Dilución / Peso molecular / Conversión de unidades / Formulación in vivo / Solubilidad

g/mol

Reviews

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