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Dibenzylfluorescein

(Synonyms: DBF, NSC 645658) 目录号 : GC43440

A fluorogenic cytochrome P450 substrate

Dibenzylfluorescein Chemical Structure

Cas No.:97744-44-0

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Sample solution is provided at 25 µL, 10mM.

Description

Dibenzylfluorescein is a fluorogenic probe that acts as a substrate for specific cytochrome P450 (CYP) isoforms, including CYP3A4, CYP2C8, CYP2C9, CYP2C19, and aromatase (CYP19). [1] [2] [3] Dibenzylfluorescein is dealkylated by these CYP isoforms to produce fluorescein benzyl ether, which is further hydrolyzed to fluorescein by the addition of base (typically 2 M NaOH). [3] Dibenzylfluorescein is typically used near its apparent Km value of 0.87-1.9 µM. [1] [2] [3] The fluorescence of fluorescein is evaluated using excitation/emission wavelengths of 485/538 nm. Dibenzylfluorescein is used to detect changes in CYP catalytic activity caused by drugs or disease.[1] [4] 

Reference:
[1]. Stresser, D.M., Blanchard, A.P., Turner, S.D., et al. Substrate-dependent modulation of CYP3A4 catalytic activity: Analysis of 27 test compounds with four fluorometric substrates. Drug Metabolism and Disposition 28(12), 1440-1448 (2000).
[2]. Donato, M.T., Jiménez, N., Castell, J.V., et al. Fluorescence-based assays for screening nine cytochrome P450 (P450) activities in intact cells expressing individual human P450 enzymes. Drug Metab. Dispos. 32(7), 699-706 (2004).
[3]. Salminen, K.A., Leppänen, J., Venäläinen, J.I., et al. Simple, direct, and informative method for the assessment of CYP2C19 enzyme inactivation kinetics. Drug Metabolism and Disposition 39(3), 412-418 (2011).
[4]. Moutinho, D., Marohnic, C.C., Panda, S.P., et al. Altered human CYP3A4 activity caused by Antley-Bixler syndrome-related variants of NADPH-cytochrome P450 oxidoreductase measured in a robust in vitro system. Drug Metabolism and Disposition 40(4), 754-760 (2012).

化学性质

Cas No. 97744-44-0 SDF
别名 DBF, NSC 645658
Canonical SMILES O=C1C=C2OC3=CC(OCC4=CC=CC=C4)=CC=C3C(C5=CC=CC=C5C(OCC6=CC=CC=C6)=O)=C2C=C1
分子式 C34H24O5 分子量 512.6
溶解度 DMF: 25 mg/ml,DMF:PBS(pH7.2) (1:2): 0.25 mg/ml,DMSO: 10 mg/ml 储存条件 Store at -20°C, protect from light
General tips 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。
储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。
Shipping Condition 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。

溶解性数据

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1 mg 5 mg 10 mg
1 mM 1.9508 mL 9.7542 mL 19.5084 mL
5 mM 0.3902 mL 1.9508 mL 3.9017 mL
10 mM 0.1951 mL 0.9754 mL 1.9508 mL
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