Resorufin benzyl ether - CAS 87687-02-3
Molecular Formula:
C19H13NO3
Molecular Weight:
303.3
COA:
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Application\Fluorophore:
Cell and Organelle Stains
Description:
Resorufin benzyl ether is a red fluorometric probe that acts as a substrate for cytochrome P450 CYP3A4. It is used to screen the inhibition/activation potential of test compounds, to predict potential drug-drug interactions, or to monitor other CYP450 activities.
Purity:
≥98%
Appearance:
Solid Powder
Synonyms:
Benzyloxyresorufin; 7-Benzyloxyresorufin; 7-(benzyloxy)-3H-phenoxazin-3-one
Storage:
Store at -20°C
MSDS:
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Excitation:
571 nm
Emission:
585 nm
1.Inhibition of CYP3A4 in a rapid microtiter plate assay using recombinant enzyme and in human liver microsomes using conventional substrates.
Nomeir AA1, Ruegg C, Shoemaker M, Favreau LV, Palamanda JR, Silber P, Lin CC. Drug Metab Dispos. 2001 May;29(5):748-53.
Cytochrome P450 inhibition studies are performed in the pharmaceutical industry in the discovery stage to screen candidates that may have the potential for clinical drug-drug interactions. A 96-well microtiter plate assay using recombinant cytochrome P450 (Supersomes) has been used to increase the overall throughput. The IC(50) values for the inhibition of CYP3A4 by 52 new chemical entities (NCEs) were determined using the Supersomes assay with resorufin benzyl ether as a substrate, and the data were compared with those obtained in human liver microsomes (HLM) using midazolam as a substrate. Among the 52 compounds tested, 25 showed IC(50) values within a 5-fold difference in the two assays. For all compounds that showed a >5-fold difference, the IC(50) values in the Supersomes assay were lower than those obtained in HLM, except for one compound. Further studies suggested that this discrepancy was not related to difference in protein concentrations between the two assays.
2.Analysis of the inhibitory potential of Ginkgo biloba, Echinacea purpurea, and Serenoa repens on the metabolic activity of cytochrome P450 3A4, 2D6, and 2C9.
Yale SH1, Glurich I. J Altern Complement Med. 2005 Jun;11(3):433-9.
OBJECTIVE: To study the potential of three top-selling herbal products, Ginkgo biloba, Echinacea purpurea, and Serenoa repens to inhibit the in vitro enzymatic activity of three of the most important drug metabolizing enzymes, cytochrome P450 (CYP) 3A4, 2D6, and 2C9.
3.Observational study of hepatic cytochrome P-450 protein expression and activity in summer flounder (Paralichtys dentatus) after combination ormetoprim-sulfadimethoxine treatment.
Topic Popovic N1, Babish JG, Bowser PR. Chemotherapy. 2007;53(5):313-5. Epub 2007 Aug 29.
The metabolism of aquaculture antibiotics on the piscine, hepatic cytochrome P-450 (CYP) system has not yet been defined. Fifty summer flounder, maintained at 20 degrees C, were fed ormetoprim-sulfadimethoxine (Romet-30(R)) at 1% body weight daily and were randomly sampled before treatment and on days 1, 6, 10 and 21 after treatment. Western blotting of hepatic microsomes included goat antirat CYP1A1 and rabbit antihuman CYP3A4 serum. Catalytic activities comprised: 3-cyano-7-ethoxycoumarin (CEC), 7-benzyloxy-4-trifluoromethylcoumarin (BFC), resorufin benzyl ether (BzRes). Treatment induced CYP1A1 and CYP3A4 expression. Dealkylation of CEC (CYP1A2) was increased after treatment. Romet-30 inhibited CYP3A4 activity measured by BFC, but induced BzRes CYP3A4. The usefulness of mammalian antibodies for piscine P-450 Western blotting was demonstrated. The hepatic P-450 1A2 and 3A4 metabolism was quantifiable by kits developed for mammalian microsomes.
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CAS 87687-02-3 Resorufin benzyl ether

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