| Bioactivity | LKY-047, a Decursin derivative, is a potent and selective reversible competitive cytochrome P45022J2 (CYP2J2) inhibitor with an IC50 of 1.7 μM. LKY-047 is inactive against other human P450s, such as CYPs 1A2, 2A6, 2B6, 2C8, 2C9, 2C19, 2D6, 2E1, and 3A[1]. | ||||||||||||
| Invitro | LKY-047 is a strong competitive inhibitor of CYP2J2-mediated astemizole O-demethylase and terfenadine hydroxylase activity, with Ki values of 0.96 μM and 2.61 μM, respectively. LKY-047 also acted as an uncompetitive inhibitor of CYP2J2-mediated ebastine hydroxylation with a Ki value of 3.61 μM[1]. At 20 μM LKY-047 concentration, approximately 20-fold greater than the Ki value, LKY-047 is found to inhibit CYP2J2 by 85.3%, and only slightly affecting the enzyme activities of the other P450s tested. LKY-047 weakly inhibits CYP2D6 enzyme activity (37.2%) at 20 μM concentration[1]. | ||||||||||||
| Name | LKY-047 | ||||||||||||
| CAS | 1954681-29-8 | ||||||||||||
| Formula | C23H19NO7 | ||||||||||||
| Molar Mass | 421.40 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
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| Reference | [1]. Nguyen Minh Phuc, et al. LKY-047: First Selective Inhibitor of Cytochrome P450 2J2. Drug Metab Dispos. 2017 Jul;45(7):765-769. |
LKY-047
CAS: 1954681-29-8 F: C23H19NO7 W: 421.40
LKY-047, a Decursin derivative, is a potent and selective reversible competitive cytochrome P45022J2 (CYP2J2) inhibitor
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