CYP2J11 Inhibitors
Chemical inhibitors of CYP2J11 act through various mechanisms to impede the enzyme's function. Terfenadine and miconazole exert their effects by targeting the potassium channels and the enzyme's heme iron, respectively. Terfenadine is known to block hERG potassium channels, which are modulated by the products of CYP2J11, leading to a reduction in the enzyme's activity. Miconazole, on the other hand, binds directly to the active site of CYP2J11, the heme group, thwarting the normal metabolization process. Ketoconazole employs a similar approach by coordinating to the heme group within CYP2J11, disrupting the enzyme's activity. Montelukast operates indirectly; it lowers the levels of leukotrienes, thereby decreasing substrate availability for CYP2J11 and consequently decreasing the enzyme's activity.
Other inhibitors, such as danazol, clotrimazole, and ticlopidine, interfere with CYP2J11 by various means. Danazol competes with natural substrates for the binding site on CYP2J11, reducing the enzyme's ability to metabolize its actual substrates. Clotrimazole impedes the enzyme's function by binding to its heme iron, which is essential for metabolic activity. Ticlopidine has a unique mechanism where it forms a reactive metabolite that irreversibly binds to CYP2J11, leading to a sustained inhibition. Diethyldithiocarbamate, chloramphenicol, sulfinpyrazone, phenylbutazone, and propylthiouracil each inhibit CYP2J11 through their interactions with the enzyme's active site or the heme group. Diethyldithiocarbamate acts as a chelating agent, binding to the heme iron and interfering with heme-iron catalyzed reactions essential to the enzyme's function. Chloramphenicol binds to the active site, obstructing the catalytic activity. Sulfinpyrazone and phenylbutazone both inhibit through competitive inhibition, directly competing with CYP2J11's substrates. Lastly, propylthiouracil inhibits the enzyme's oxidizing ability, affecting the metabolism of substrates by CYP2J11.
Items 1 to 10 of 11 total
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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 a known blocker of hERG potassium channels. CYP2J11, being a cytochrome P450 enzyme involved in the metabolism of arachidonic acid to epoxygenase metabolites, is implicated in the regulation of cardiac ion channels similar to hERG. Terfenadine inhibition of these channels can lead to reduced function of CYP2J11 as the enzyme's products modulate these channels. | ||||||
Miconazole | 22916-47-8 | sc-204806 sc-204806A | 1 g 5 g | $66.00 $160.00 | 2 | |
Miconazole is an imidazole antifungal agent that inhibits several cytochrome P450 enzymes. It can inhibit CYP2J11 by binding to the heme iron within the enzyme's active site, preventing the normal metabolization process of its substrates. | ||||||
Ketoconazole | 65277-42-1 | sc-200496 sc-200496A | 50 mg 500 mg | $63.00 $265.00 | 21 | |
Ketoconazole is a broad cytochrome P450 inhibitor. It can inhibit CYP2J11 by coordinating to the heme group in the enzyme, thereby interfering with enzyme activity and substrate metabolism. | ||||||
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, a leukotriene receptor antagonist, can inhibit CYP2J11 by reducing the availability of leukotrienes, which are products of the arachidonic acid pathway and substrates for various P450 enzymes, leading to a decrease in substrate availability for CYP2J11 activity. | ||||||
Danazol | 17230-88-5 | sc-203021 sc-203021A | 100 mg 250 mg | $92.00 $238.00 | 3 | |
Danazol is a synthetic steroid that can inhibit various P450 enzymes by competing with endogenous substrates for the active site, including CYP2J11, potentially inhibiting its activity by substrate competition. | ||||||
Chloramphenicol | 56-75-7 | sc-3594 | 25 g | $90.00 | 10 | |
Chloramphenicol is an antibiotic known to inhibit cytochrome P450 enzymes. It can inhibit CYP2J11 by binding to the active site and interfering with the enzyme's catalytic activity. | ||||||
Clotrimazole | 23593-75-1 | sc-3583 sc-3583A | 100 mg 1 g | $42.00 $57.00 | 6 | |
Clotrimazole, an antifungal drug, can inhibit CYP2J11 by binding to the enzyme's heme iron, which is pivotal for the enzyme's catalytic activity, thus impeding the metabolism of CYP2J11 substrates. | ||||||
Ticlopidine Hydrochloride | 53885-35-1 | sc-205861 sc-205861A | 1 g 5 g | $32.00 $99.00 | 2 | |
Ticlopidine is a known inhibitor of cytochrome P450 enzymes, including CYP2J11. It can form a reactive metabolite that irreversibly binds to the P450 enzyme, leading to inhibition of its metabolic activity. | ||||||
(±)-Sulfinpyrazone | 57-96-5 | sc-202822 sc-202822A | 1 g 5 g | $42.00 $94.00 | 2 | |
Sulfinpyrazone is a uricosuric agent that inhibits the activity of several cytochrome P450 enzymes. It can inhibit CYP2J11 by competitive inhibition, where it directly competes with the natural substrates of the enzyme. | ||||||
Phenylbutazone | 50-33-9 | sc-204843 | 5 g | $32.00 | 1 | |
Phenylbutazone is an anti-inflammatory drug that can inhibit certain P450 enzymes. It may inhibit CYP2J11 by competitive inhibition, as it can bind to the enzyme's active site and prevent substrate metabolism. | ||||||