Date published: 2025-10-18

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CYP3A4 Activators

CYP3A4 stands as one of the most significant enzymes within the vast cytochrome P450 superfamily, playing a pivotal role in the metabolism of xenobiotics, which includes a wide variety of drugs, toxins, and other foreign compounds. Primarily found in the liver but also present in the intestines, CYP3A4 catalyzes the oxidation of organic substances, facilitating their biotransformation and subsequent elimination from the body. Due to its central role in drug metabolism, CYP3A4 is often the focus of pharmacokinetic studies, with its activity having profound implications on drug bioavailability, efficacy, and for drug-drug interactions. The enzyme's function is characterized by its broad substrate specificity, enabling it to metabolize a wide array of compounds, a feature that underscores its importance in detoxification processes. CYP3A4 activators are chemical entities that enhance the activity or expression of the CYP3A4 enzyme. These activators can function by directly increasing the enzymatic activity or by upregulating the transcription of the CYP3A4 gene. The presence of activators can lead to an accelerated metabolism of substances that are substrates for CYP3A4, altering the pharmacokinetics of these compounds in the body. The mechanism by which different activators function can be multifaceted, involving direct interactions with the enzyme, modulation of signaling pathways that regulate CYP3A4 expression, or alterations in cellular environments that favor enhanced enzyme activity. As the scientific community delves deeper into the intricacies of metabolic pathways, the understanding of CYP3A4 activators and their implications on xenobiotic metabolism remains a focal point, illustrating the complexity of biochemical interactions within the body.

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Items 1 to 10 of 12 total

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Product NameCAS #Catalog #QUANTITYPriceCitationsRATING

α-Naphthoflavone

604-59-1sc-257037
sc-257037A
sc-257037B
sc-257037C
1 g
5 g
25 g
100 g
$33.00
$45.00
$153.00
$490.00
3
(1)

α-Naphthoflavone is a notable compound that interacts with CYP3A4 through its planar aromatic structure, which allows for effective π-π stacking with the enzyme's active site. This interaction can modulate the enzyme's conformation, influencing substrate access and catalytic turnover. Additionally, its ability to form hydrogen bonds with key amino acid residues enhances binding affinity, potentially altering metabolic pathways and enzyme kinetics in a unique manner.

Rifampicin

13292-46-1sc-200910
sc-200910A
sc-200910B
sc-200910C
1 g
5 g
100 g
250 g
$95.00
$322.00
$663.00
$1438.00
6
(1)

Induces CYP3A4 by activating the pregnane X receptor (PXR), a nuclear receptor that upregulates CYP3A4 transcription.

Dexamethasone

50-02-2sc-29059
sc-29059B
sc-29059A
100 mg
1 g
5 g
$76.00
$82.00
$367.00
36
(1)

Acts via the glucocorticoid receptor and can also activate PXR to induce CYP3A4 expression.

Hyperforin

11079-53-1sc-507549
250 µg
$420.00
(0)

Induces CYP3A4 through activation of PXR.

Carbamazepine

298-46-4sc-202518
sc-202518A
1 g
5 g
$32.00
$70.00
5
(0)

Induces CYP3A4 via activation of both PXR and CAR.

Efavirenz

154598-52-4sc-207612
10 mg
$168.00
3
(1)

Induces CYP3A4 primarily through activation of PXR.

Nevirapine

129618-40-2sc-208092
5 mg
$97.00
5
(1)

An antiretroviral suggested compound that can induce CYP3A4 via PXR activation.

5-Pregnen-3β-ol-20-one-16α-carbonitrile

1434-54-4sc-227010
50 mg
$68.00
3
(1)

Rodent-specific CYP3A inducer acting through PXR activation.

Pioglitazone

111025-46-8sc-202289
sc-202289A
1 mg
5 mg
$54.00
$123.00
13
(1)

While primarily an activator of PPARγ, it can also influence CYP3A4 expression.

Omeprazole

73590-58-6sc-202265
50 mg
$66.00
4
(1)

Proton pump inhibitor that can induce CYP3A4, potentially through PXR or other mechanisms.