CYP2B6 Activators
The class of chemicals known as CYP2B6 activators encompasses a diverse range of compounds that indirectly upregulate the activity of the CYP2B6 enzyme, a key player in drug metabolism. These chemicals achieve their effects by modulating various cellular receptors and transcription factors, leading to enhanced expression and activity of CYP2B6. One prominent mechanism involves the activation of nuclear receptors such as the constitutive androstane receptor (CAR) and the pregnane X receptor (PXR). Chemicals like phenobarbital and rifampicin bind to these receptors, triggering a cascade of intracellular events that culminate in the increased transcription of CYP2B6 genes. This transcriptional upregulation directly boosts the enzyme's expression and its subsequent metabolic capacity.
Another pathway involves the peroxisome proliferator-activated receptor alpha (PPARα), targeted by compounds like clofibrate. Activation of PPARα leads to similar outcomes, enhancing CYP2B6 expression and its role in metabolizing a variety of substrates. Additionally, certain anticonvulsants, like carbamazepine and phenytoin, and even some herbal supplements such as St. John's Wort, act on these receptors, demonstrating the broad spectrum of chemicals that can indirectly influence CYP2B6 activity.
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| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
Rifampicin | 13292-46-1 | sc-200910 sc-200910A sc-200910B sc-200910C | 1 g 5 g 100 g 250 g | $97.00 $328.00 $676.00 $1467.00 | 6 | |
Rifampicin, an antibiotic, acts as an inducer of CYP2B6 by activating the pregnane X receptor (PXR). PXR, when stimulated, binds to specific DNA sequences, promoting the transcription of genes including CYP2B6, thus elevating its expression and metabolic activity. | ||||||
Clofibrate | 637-07-0 | sc-200721 | 1 g | $33.00 | ||
Clofibrate, a fibric acid derivative, upregulates CYP2B6 activity through peroxisome proliferator-activated receptor alpha (PPARα) activation. Activation of PPARα leads to an increase in CYP2B6 gene transcription, enhancing its enzymatic activity in metabolizing various substrates. | ||||||
Carbamazepine | 298-46-4 | sc-202518 sc-202518A | 1 g 5 g | $33.00 $71.00 | 5 | |
Carbamazepine, an anticonvulsant, induces CYP2B6 by activating both CAR and PXR receptors. This dual activation leads to an increase in the transcription and expression of CYP2B6, thereby amplifying its metabolic capacity. | ||||||
Omeprazole | 73590-58-6 | sc-202265 | 50 mg | $67.00 | 4 | |
Omeprazole, a proton pump inhibitor, has been shown to influence CYP2B6 expression. While its mechanism is not fully understood, it appears to interact with hepatic transcription factors, potentially including PXR, thus modifying CYP2B6 activity. | ||||||
Ketoconazole | 65277-42-1 | sc-200496 sc-200496A | 50 mg 500 mg | $63.00 $265.00 | 21 | |
Ketoconazole, an antifungal agent, is known to modulate various cytochrome P450 enzymes, including CYP2B6. Its exact mechanism on CYP2B6 is not fully elucidated but involves interaction with liver receptors impacting CYP2B6 expression. | ||||||
Dexamethasone | 50-02-2 | sc-29059 sc-29059B sc-29059A | 100 mg 1 g 5 g | $91.00 $139.00 $374.00 | 36 | |
Dexamethasone, a corticosteroid, induces CYP2B6 expression through glucocorticoid receptor-mediated mechanisms. This interaction influences the transcription and expression of CYP2B6 in hepatic cells, enhancing its metabolic function. | ||||||