CYP2J9 Inhibitors
Chemical inhibitors of CYP2J9 include a variety of compounds that interact with the enzyme in different ways to impede its function. Terfenadine and Astemizole are two such inhibitors that bind directly to the catalytic site of CYP2J9. This binding prevents the enzyme from metabolizing other substrates that would normally be processed. Similar in their mode of action, Danazol and Amiodarone also bind to the active site of CYP2J9, thereby inhibiting its natural catalytic function. Ketoconazole exhibits its inhibitory effect by binding to the heme iron within the active site of CYP2J9, which is crucial for the enzyme's activity. The heme iron is a central component of the cytochrome P450 enzymes, and its obstruction leads to a significant decrease in enzyme activity.
Further extending the list of CYP2J9 inhibitors, Troleandomycin inhibits the enzyme by forming a stable metabolic intermediate complex with the heme iron within the active site, which blocks the enzyme's catalytic function. Miconazole and Sulconazole, both antifungal agents, are known to interact with the heme group of CYP2J9, leading to diminished enzymatic activity. Fluconazole, Itraconazole, and Clotrimazole also inhibit CYP2J9 through a similar mechanism of heme iron binding, which is integral to the enzyme's function. Lastly, Propiconazole, another antifungal agent, inhibits CYP2J9 by occupying its active site, which prevents the enzyme from engaging in the metabolism of other compounds. Each of these chemicals demonstrates a capacity to inhibit CYP2J9 by interacting with specific sites crucial for the enzyme's metabolic processing capability.
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| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
Terfenadine | 50679-08-8 | sc-208421A sc-208421B sc-208421 | 500 mg 1 g 5 g | $44.00 $71.00 $120.00 | ||
Terfenadine is known to be metabolized by cytochrome P450 enzymes. CYP2J9, being a member of this family, is involved in the metabolic processing of drugs. Terfenadine could cause competitive inhibition for CYP2J9 as it occupies the active site, thereby preventing the metabolism of other substrates by this enzyme. | ||||||
Danazol | 17230-88-5 | sc-203021 sc-203021A | 100 mg 250 mg | $92.00 $238.00 | 3 | |
Danazol is metabolized by cytochrome P450 enzymes and can inhibit CYP2J9 by binding to the enzyme's active site. This binding can prevent the enzyme from catalyzing its natural reactions, leading to functional inhibition of CYP2J9. | ||||||
Amiodarone | 1951-25-3 | sc-480089 | 5 g | $318.00 | ||
Amiodarone is a known inhibitor of several cytochrome P450 enzymes, and it can inhibit CYP2J9 by binding to the enzyme's active site, which prevents the typical enzymatic activity of CYP2J9. | ||||||
Ketoconazole | 65277-42-1 | sc-200496 sc-200496A | 50 mg 500 mg | $63.00 $265.00 | 21 | |
Ketoconazole is a broad cytochrome P450 inhibitor that can inhibit CYP2J9 by binding to its heme iron, an essential component of the active site. This binding inhibits the enzyme's activity by blocking the access of natural substrates. | ||||||
Miconazole | 22916-47-8 | sc-204806 sc-204806A | 1 g 5 g | $66.00 $160.00 | 2 | |
Miconazole inhibits cytochrome P450 enzymes by interacting with their heme group. It could inhibit CYP2J9 by this mechanism, leading to a decrease in the enzyme's metabolic activity. | ||||||
Sulconazole | 61318-90-9 | sc-338599 | 100 mg | $1000.00 | 1 | |
Sulconazole is an imidazole antifungal agent known to inhibit cytochrome P450-dependent enzymes. It may inhibit CYP2J9 by binding to the enzyme's heme iron, which is pivotal for its enzymatic function. | ||||||
Fluconazole | 86386-73-4 | sc-205698 sc-205698A | 500 mg 1 g | $54.00 $84.00 | 14 | |
Fluconazole is a potent inhibitor of cytochrome P450 enzymes and can inhibit CYP2J9 by binding to the heme iron within the catalytic site, which is essential for enzymatic activity. | ||||||
Itraconazole | 84625-61-6 | sc-205724 sc-205724A | 50 mg 100 mg | $78.00 $142.00 | 23 | |
Itraconazole can inhibit CYP2J9 by binding to the heme group in the enzyme's active site, which prevents the normal metabolic activity of the enzyme. | ||||||
Clotrimazole | 23593-75-1 | sc-3583 sc-3583A | 100 mg 1 g | $42.00 $57.00 | 6 | |
Clotrimazole is known to inhibit cytochrome P450 enzymes by binding to the heme component of the enzyme. This binding inhibits the enzyme's activity, including that of CYP2J9, by blocking the interaction with its substrates. | ||||||