A potent CYP3A4 inhibitor (IC50s = 0.30 ppm in a cell-free assay

6’,7’-Epoxybergamottin – 5 mg

Brand:
Cayman
CAS:
206978-14-5
Storage:
-20
UN-No:
Non-Hazardous - /

6’7′-Epoxybergamottin is a furanocoumarin found in grapefruit.{40136} It is a potent inhibitor of the cytochrome P450 (CYP) isoform CYP3A4 with an IC50 value of 0.30 ppm in a cell-free assay, 0.33 µM in HL7 human liver cells, and 0.22 µM in S9 human intestine cells.{40137} It has been studied in the context of drug interactions with grapefruit constituents. It is found in grapefruit juice at concentrations of 0.1-7.4 µM and inhibits the transport of talinolol (Item No. 16116), a permeability glycoprotein (P-gp/ABCB1) transporter substrate, across Caco-2 cell monolayers (IC50 = 0.7 µM).{40135} 6’7’-Epoxybergamottin also has insecticidal properties with a concentration of 5 µg/cm2 leading to 100% mortality of adult olive fruit flies.{40138}  

 

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Description

A potent CYP3A4 inhibitor (IC50s = 0.30 ppm in a cell-free assay, 0.33 µM in HL7 human liver cells, and 0.22 µM in S9 human intestine cells); inhibits the transport of talinolol, a P-gp/ABCB1 transporter substrate, across Caco-2 cell monolayers (IC50 = 0.7 µM); has insecticidal properties (5 µg/cm2 leads to 100% mortality of adult olive fruit flies)

Formal name: 4-[[(2E)-5-(3,3-dimethyl-2-oxiranyl)-3-methyl-2-penten-1-yl]oxy]-7H-furo[3,2-g][1]benzopyran-7-one

Synonyms:  Epoxybergamottin

Molecular weight: 354.4

CAS: 206978-14-5

Purity: ≥98%

Formulation: A crystalline solid

Application|Mass Spectrometry||Product Type|Biochemicals|Natural Products|Coumarins||Product Type|Biochemicals|Pesticides|Insecticides||Product Type|Biochemicals|Small Molecule Inhibitors|Cytochrome P450||Product Type|Biochemicals|Small Molecule Inhibitors|MMPs||Research Area|Toxicology|Drug Metabolism|Cytochrome P450

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