197226
BCRP Inhbitor
N-(4-(2-hydroxyethyl)phenyl)-2-(4-nitrobenzamido)benzamide
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Merck KGaA
Frankfurter Str. 250
64293 Darmstadt
Germany
Telefon: +49 6151 72-0
Faks: +49 6151 72 2000
31 May 2012
memuat
A non-tetrahydroisoquinoline BCRP specific inhibitor based on the anthranilic acid scaffold, that displays an IC50 of 1.39 µM in a Hoechst 33343 assay in stably transfected MDCK BCRP cells, which is ˜50-fold more potent than novobiocin (IC50 = 65 µM), and shows no effect towards other ATP binding cassette (ABC) transporters P-gp and MRP1 at up to a concentration of 10 µM. It is shown to be an allosteric inhibitor in enzyme kinetics assays in the presence of BCRP specific substrates pheophorbide A and imitanib, and does not lead to a decrease in cell viability up to a concentration of 10 µM.
| Informasi produk | |||
|---|---|---|---|
| Form | Off-white solid | ||
| Protect from Light | Ya | ||
| Packaged under inert gas | Ya | ||
| Purity | ≥95% by HPLC | ||
| Formulasi kimia | C22H19N3O5 | ||
| Simpan dan kirim informasi | |||
|---|---|---|---|
| Penyimpanan | +2°C to +8°C | ||
| Ship |
Ambient Temperature Only
Standard Handling |
||
