This compound is a customized synthesis product. We have a strong synthesis team with excellent synthesis technology and capabilities. However, due to various objective factors, there is a low probability that the synthesis will not be successful. If you need to learn more, please feel free to consult us, we will serve you wholeheartedly.
This compound is a customized synthesis product. We have a strong synthesis team with excellent synthesis technology and capabilities. However, due to various objective factors, there is a low probability that the synthesis will not be successful. If you need to learn more, please feel free to consult us, we will serve you wholeheartedly.
LKY-047
Catalog No. T39371 CAS
1954681-29-8
LKY-047, a derivative of Decursin, is a highly effective and specific reversible competitive inhibitor of cytochrome P45022J2 (CYP2J2), with an IC 50 value of 1.7 μM. LKY-047 does not display inhibitory activity against other human P450 enzymes including CYPs 1A2, 2A6, 2B6, 2C8, 2C9, 2C19, 2D6, 2E1, and 3A.
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LKY-047, a derivative of Decursin, is a highly effective and specific reversible competitive inhibitor of cytochrome P45022J2 (CYP2J2), with an IC 50 value of 1.7 μM. LKY-047 does not display inhibitory activity against other human P450 enzymes including CYPs 1A2, 2A6, 2B6, 2C8, 2C9, 2C19, 2D6, 2E1, and 3A.
Targets&IC50
CYP2J2:1.7 μM (IC50)
In vitro
LKY-047 is a potent inhibitor of CYP2J2, specifically targeting astemizole O-demethylase and terfenadine hydroxylase activities, with inhibition constants (K_i values) of 0.96 μM and 2.61 μM, respectively. It also serves as an uncompetitive inhibitor against CYP2J2-mediated ebastine hydroxylation, with a K_i of 3.61 μM[1]. At a concentration of 20 μM, significantly higher than its K_i values, LKY-047 inhibits CYP2J2 activity by 85.3%, demonstrating substantial selectivity by only minimally affecting the activities of other tested P450 enzymes. It exhibits a moderate inhibitory effect on CYP2D6, with 37.2% activity reduction at the same concentration[1].
Molecular Weight
421.405
Formula
C23H19NO7
CAS No.
1954681-29-8
Storage
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Method for preparing DMSO master liquid: mg
drug pre-dissolved in μL DMSO (Master liquid concentration
mg/mL),
Method for preparing in vivo formulation:Take μL
DMSO master liquid, next add μL PEG300, mix and clarify, next add μL
Tween 80,mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation:Take μL
DMSO master liquid, next add μL Corn oil,mix and clarify.
Note:
Be sure to add the solvent(s) in order. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
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Tech Support
Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.