GLPBio

N-Nornuciferine

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

製品は研究用途にのみ使用できます。人体には使用できません。患者への販売は行っておりません。

N-Nornuciferine
Cas No.: 4846-19-9
5mgIn Stock
$213.00
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10mgIn Stock
$367.00
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製品説明 (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.

実験プロトコル (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.

製品資料 (Product Documents)

Purity:>98.00%Appearance:A solid
COASDSData Sheet

化学的性質 (Chemical Properties)

CAS番号
4846-19-9
同義語
Daechualkaloid E, (R)-Nornuciferine, (-)-Nornuciferine, Sanjoinine Ia
SMILES
COC1=C(OC)C2=C3C(CCN[C@]3([H])CC4=CC=CC=C24)=C1
分子式
C18H19NO2
分子量
281.35
溶解性
DMSO : 100 mg/mL (355.43 mM; Need ultrasonic)
保存条件
Store at -20°C,protect from light
一般的な注意事項
製品の溶解性データに基づいて適切な溶媒を選択してください。調製後は、凍結融解の繰り返しを避けるため、ストック溶液を小分けしてください。
ストック溶液は、-80°Cで保存する場合は6か月以内、-20°Cで保存する場合は1か月以内に使用してください。
溶解性を高めるには、チューブを37°Cに温め、適切な時間超音波処理してください。
配送条件
評価用サンプルは保冷剤とともに発送します。その他の容量は室温で発送し、ご要望に応じて保冷剤を同梱します。

計算ツール (Calculators)モル濃度 / 希釈 / 分子量 / 単位変換 / in vivo製剤 / 溶解度

g/mol

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