CYP2J13 Inhibitors
Chemical inhibitors of CYP2J13 can impede the protein's normal function through various modes of interaction. Montelukast and Zileuton, both acting on pathways related to arachidonic acid metabolism, indirectly reduce the activity of CYP2J13. Montelukast, a leukotriene receptor antagonist, interferes with the leukotriene pathway that is upstream of the CYP2J13's role in arachidonic acid metabolism. By reducing the inflammatory response, there is a consequent decrease in the production of compounds that CYP2J13 would typically metabolize. Zileuton, by inhibiting the 5-lipoxygenase enzyme, blocks the conversion of arachidonic acid to leukotrienes, thus lowering the availability of arachidonic acid for CYP2J13 to process.
The other group of inhibitors, including Ketoconazole, Miconazole, Itraconazole, Fluconazole, Voriconazole, Sulconazole, Tioconazole, Econazole, Clotrimazole, and Metronidazole, directly target the catalytic activity of CYP2J13. Ketoconazole and Miconazole achieve inhibition by binding to the heme iron within the active site of CYP2J13, a crucial component for the enzymatic activity. This binding effectively halts the metabolism of substrates by CYP2J13. Similarly, Itraconazole, another antifungal compound, inhibits the protein by binding to its heme iron, disrupting the normal catalytic process. Fluconazole and Voriconazole, both triazole compounds, compete with CYP2J13's natural substrates for binding at the active site, reducing the metabolism of these substrates. Sulconazole, Tioconazole, and Econazole, while differing in molecular structure, also act as imidazole antifungals that inhibit the function of CYP2J13 by occupying its active site. Clotrimazole binds to the enzyme's heme group, essential for the protein's function, thereby inhibiting its activity. Lastly, Metronidazole, known for its antibiotic and antiprotozoal properties, competitively binds to CYP2J13, impeding its enzymatic function. Each of these compounds can attenuate the activity of CYP2J13 through their respective mechanisms of binding and inhibition.
| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
Montelukast Sodium | 151767-02-1 | sc-202231 sc-202231A sc-202231B | 10 mg 25 mg 250 mg | $51.00 $85.00 $161.00 | 5 | |
Montelukast is a leukotriene receptor antagonist that inhibits the function of leukotrienes in the inflammatory pathway. CYP2J13 is involved in the metabolism of arachidonic acid to epoxyeicosatrienoic acids (EETs), which are signaling molecules that can be involved in inflammatory processes. By inhibiting leukotriene function, Montelukast reduces the inflammatory response, which in turn can decrease the production of EETs and thus inhibit the catalytic activity of CYP2J13 which is required for their formation. | ||||||
Zileuton | 111406-87-2 | sc-204417 sc-204417A sc-204417B sc-204417C | 10 mg 50 mg 1 g 75 g | $84.00 $307.00 $369.00 $1254.00 | 8 | |
Zileuton is a 5-lipoxygenase inhibitor that blocks the formation of leukotrienes from arachidonic acid. Since CYP2J13 is involved in metabolizing arachidonic acid, the inhibition of the leukotriene pathway by Zileuton can reduce the overall turnover of arachidonic acid, thereby reducing the substrate availability for CYP2J13 and effectively inhibiting its activity. | ||||||
Ketoconazole | 65277-42-1 | sc-200496 sc-200496A | 50 mg 500 mg | $63.00 $265.00 | 21 | |
Ketoconazole is a broad-spectrum antifungal agent known to inhibit cytochrome P450 enzymes. It can inhibit CYP2J13 by binding to its heme iron, which is essential for the enzyme's catalytic activity, thus directly inhibiting the enzyme's ability to metabolize its substrates. | ||||||
Miconazole | 22916-47-8 | sc-204806 sc-204806A | 1 g 5 g | $66.00 $160.00 | 2 | |
Miconazole, another antifungal agent, also inhibits cytochrome P450 enzymes by interacting with the heme group. By binding to the heme iron within CYP2J13, Miconazole prevents the enzymatic activity of CYP2J13, leading to an inhibition of its metabolic functions. | ||||||
Itraconazole | 84625-61-6 | sc-205724 sc-205724A | 50 mg 100 mg | $78.00 $142.00 | 23 | |
Itraconazole is an antifungal compound that can inhibit cytochrome P450 enzymes by binding to the enzyme's heme iron. Itraconazole's interaction with CYP2J13 disrupts its normal catalytic process, thereby inhibiting the enzyme's activity. | ||||||
Fluconazole | 86386-73-4 | sc-205698 sc-205698A | 500 mg 1 g | $54.00 $84.00 | 14 | |
Fluconazole is a triazole antifungal drug that can inhibit CYP2J13 by competing with the natural substrates for the binding at the active site. This competition reduces the enzymatic activity of CYP2J13 by preventing the metabolism of its substrates. | ||||||
Sulconazole | 61318-90-9 | sc-338599 | 100 mg | $1000.00 | 1 | |
Sulconazole, an imidazole antifungal, is known to inhibit cytochrome P450 enzymes. It binds to the active site of CYP2J13, thereby inhibiting the enzyme's function. | ||||||
Econazole | 27220-47-9 | sc-279013 | 5 g | $240.00 | ||
Econazole is an imidazole antifungal agent that inhibits cytochrome P450 enzymes by binding to their heme group. This binding within CYP2J13 inhibits its catalytic activity and disrupts its metabolic functions. | ||||||
Clotrimazole | 23593-75-1 | sc-3583 sc-3583A | 100 mg 1 g | $42.00 $57.00 | 6 | |
Clotrimazole, an imidazole antifungal, can inhibit CYP2J13 by binding to the heme iron of the enzyme, which is crucial for its enzymatic activity, thus directly inhibiting the metabolism of CYP2J13 substrates. | ||||||
Metronidazole | 443-48-1 | sc-204805 sc-204805A | 5 g 25 g | $84.00 $205.00 | 11 | |
Metronidazole is an antibiotic and antiprotozoal medication that can inhibit cytochrome P450 enzymes. It does so by competitive binding to the enzyme, including CYP2J13, which inhibits its activity. | ||||||