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Chemical Structure : LKY-047
Catalog No.: PC-20617Not For Human Use, Lab Use Only.
LKY-047 (LKY047) is a potent, highly selective and reversible competitive cytochrome P450 CYP2J2 (CYP2J2) inhibitor with IC50 of 1.7 uM.
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LKY-047 (LKY047) is a potent, highly selective and reversible competitive cytochrome P450 CYP2J2 (CYP2J2) inhibitor with IC50 of 1.7 uM.
LKY-047 is a strong competitive inhibitor of CYP2J2-mediated astemizole O-demethylase and terfenadine hydroxylase activity, with Ki values of 0.96 and 2.61 μM, respectively.
LKY-047 also acts as an uncompetitive inhibitor of CYP2J2-mediated ebastine hydroxylation with a Ki value of 3.61 μM.
LKY-047 displays no inhibitory effect on other human P450s, such as CYPs 1A2, 2A6, 2B6, 2C8, 2C9, 2C19, 2D6, 2E1, and 3A (IC50 > 50 uM).
LKY-047 is useful as a selective CYP2J2 inhibitor in P450 reaction phenotyping studies and the biologic function study of this enzyme.
| M.Wt | 421.41 | |
| Formula | C23H19NO7 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Nguyen Minh Phuc, et al. Drug Metab Dispos. 2017 Jul;45(7):765-769.
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