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Chemical Structure : LKY-047
Catalog No.: PC-61747Not For Human Use, Lab Use Only.
LKY-047 is a decursin derivative that potently and selectively inhibits CYP2J2, competitively inhibits CYP2J2-mediated astemizole O-demethylase and terfenadine hydroxylase activity with Ki of 0.96 and 2.61 uM, respectively.
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LKY-047 is a decursin derivative that potently and selectively inhibits CYP2J2, competitively inhibits CYP2J2-mediated astemizole O-demethylase and terfenadine hydroxylase activity with Ki of 0.96 and 2.61 uM, respectively; also acts as an uncompetitive inhibitor of CYP2J2-mediated ebastine hydroxylation with Ki of 3.61 uM; dispalys no inhibitory effect on other human P450s, such as CYPs 1A2, 2A6, 2B6, 2C8, 2C9, 2C19, 2D6, 2E1, and 3A (IC50 >50 uM); a selective CYP2J2 inhibitor with potential application in the identification of P450 isoforms responsible for drug metabolism in reaction phenotyping assays.
| M.Wt | 421.405 | |
| Formula | C23H19NO7 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Phuc NM, et al. Drug Metab Dispos. 2017 Jul;45(7):765-769.
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