Cytochrome P450

Cat. No.

A10293

CAS No.

201530-41-8

Deferasirox

Synonyms: ICL-670; ICL-670A; CGP-72670

Deferasirox is a rationally-designed oral iron chelator, also a cytochrome P450 3A4 inducer, Cytochrome P450 2C8 inhibitor, and Cytochrome P450 1A2 inhibitor.

Cat. No.

A13361

CAS No.

1614-12-6

ABT

Synonyms: 1-Aminobenzotriazole

ABT (1-Aminobenzotriazole )is a suicide substrate for (CYP)cytochrome P-450 and chloroperoxidase.

Cat. No.

A13365

CAS No.

117620-77-6

3-Cyano-7-ethoxycoumarin

Synonyms: 7-Ethoxycoumarin-3-carbonitrile

3-Cyano-7-ethoxycoumarin is a fluorogenic substrate suitable for the continuous determination of cytochrome P450 mixed-function monooxygenases. It is a fluorescent probe useful in microsomal dealkylase studies.

Cat. No.

A13366

CAS No.

50-12-4

Mephenytoin

Mephenytoin is a CYP2C19 substrate. Anticonvulsant.

Cat. No.

A13367

CAS No.

5725-89-3

Methoxyresorufin

Synonyms: Resorufin methyl ether

Methoxyresorufin is a fluorometric substrate for cytochrome P450 linked enzymes.

Cat. No.

A20360

CAS No.

197913-15-8

CDD3506

CDD3506 is used for elevating high density lipoprotein cholesterol (HDL) by inducing hepatic cytochrome P450IIIA (CYP3A) activity.

Cat. No.

A20364

CAS No.

173865-33-3

CDD3505

CDD3505 is used for elevating high density lipoprotein cholesterol (HDL) by inducing hepatic cytochrome P450IIIA (CYP3A) activity.

Cat. No.

A21644

CAS No.

625095-61-6

Pradefovir mesylate

Synonyms: Remofovir mesylate

Pradefovir mesylate is a good substrate for liver CYP3A4. Pradefovir is converted to 9-(2-phosphonylmethoxyethyl)adenine (PMEA) in human liver microsomes with a Km of 60 μM.

Cat. No.

A37721

CAS No.

1107-26-2

β-Apo-8'-carotenal

Synonyms: Apocarotenal

β-Apo-8'-carotenal is a potent inducer of CYP1A, acting through the aryl hydrocarbon receptor (AhR) pathway. This carotenoid has demonstrated the ability to induce DNA strand breaks and lipid peroxidation in cancer cells, making it a valuable tool for research into cancer biology and metabolic disorders. Its role as a provitamin A compound further emphasizes its potential applications in studies related to cellular metabolism and disease mechanisms.

Cat. No.

A43722

CAS No.

587-98-4

Acid Yellow 36

Synonyms: Metanil Yellow

Acid Yellow 36, an azo dye and pH indicator, primarily functions as a cytochrome P450 inducer. It exhibits a color change from red at pH 1.2 to yellow at pH 2.3, making it useful in various industrial applications, including leather, paper, and textiles. In the realm of biochemical research, Acid Yellow 36 is employed to induce specific isozymes of cytochrome P450 and various cytosolic enzymes, facilitating studies on enzyme regulation and metabolism.

Cat. No.

A44982

CAS No.

2039-67-0

3-Methoxyphenylethylamine

3-Methoxyphenylethylamine is a substrate for cytochrome P450 2D6 (CYP2D6), playing a crucial role in drug metabolism. It is commonly used in research to investigate the metabolic pathways and enzyme interactions involving CYP2D6, making it valuable for studies on pharmacokinetics and drug-drug interactions. Additionally, this compound serves as an important intermediate in the synthesis of pharmaceuticals and other organic materials, furthering its applications in chemical research.

Cat. No.

A64118

CAS No.

55673-89-7

1,2,3,4,7,8,9-Heptachlorodibenzofuran

Synonyms: 1,2,3,4,7,8,9-HpCDF

1,2,3,4,7,8,9-Heptachlorodibenzofuran is a potent inducer of CYP1A1 and CYP1B1 gene expression in human peripheral blood lymphocytes, promoting aryl hydrocarbon receptor repressor (AhRR) transcription. This compound enhances ethoxyresorufin-O-deethylase (EROD) activity, serving as a reliable biomarker for CYP1A1 activation. Additionally, it displays immunosuppressive properties by decreasing the number of splenic plaque-forming cells in mice while increasing aryl hydrocarbon hydroxylase (AHH) activity in liver microsomes. 1,2,3,4,7,8,9-Heptachlorodibenzofuran is valuable for research in immunology, metabolic disorders, and environmental toxicology.

Cat. No.

A68952

CAS No.

516-15-4

11-Ketoprogesterone

Synonyms: 11KP4

11-Ketoprogesterone (11KP4) serves as a substrate for the enzymes CYP17A1 and 11β-HSD2, facilitating the conversion to 21-deoxycortisone (21dE) and 21-deoxycortisol (21dF), both of which exhibit glucocorticoid activity. This compound is pivotal for studies examining steroidogenesis and adrenal hormone metabolism. It is utilized in research applications focusing on hormonal regulation and related disorders, providing insights into steroid hormone biosynthesis pathways.

Cat. No.

A69734

CAS No.

186299-00-3

hCYP3A4 Fluorogenic substrate 1

hCYP3A4 Fluorogenic Substrate 1 is a potent substrate designed for human cytochrome P450 3A4 (hCYP3A4), exhibiting a Km value of 0.36 μM. This substrate is valuable for investigating hCYP3A4-mediated biotransformation processes and can be utilized in both cellular and in vivo imaging studies to monitor enzyme activity. Its fluorogenic properties facilitate real-time observation of metabolic activity, aiding in drug metabolism and pharmacokinetic research.

Cat. No.

A69756

CAS No.

328087-38-3

Phortress

Synonyms: NSC 710305

Phortress is a potent cytochrome P450 inducer that specifically activates the aryl hydrocarbon receptor (AhR). By eliciting the transcription of CYP1A1, it demonstrates robust antitumor activity. This compound is valuable for research applications focused on drug metabolism, environmental toxicology, and the modulation of xenobiotic responses.

Cat. No.

A69781

CAS No.

130606-60-9

N-Desmethyl diltiazem hydrochloride

N-Desmethyl diltiazem hydrochloride is a substrate for the enzyme CYP3A7, which is predominantly expressed during fetal development and has minimal expression in adult tissues. This compound is utilized in pharmacokinetic studies to investigate drug metabolism pathways in neonatal and fetal contexts. Its involvement in CYP3A7 activity makes it an important reagent for researchers examining developmental pharmacology and drug interactions.

Cat. No.

A69801

CAS No.

2318-18-5

Senkirkin

Synonyms: Senkirkine; Renardin

Senkirkin is a pyrrolizidine alkaloid that serves as a substrate for the cytochrome P450 enzyme CYP3A4. It has been shown to induce chromosomal damage in lymphocytes, highlighting its potential utility in toxicological studies. This compound can be leveraged in research applications involving drug metabolism and the assessment of genotoxicity.

Cat. No.

A69808

CAS No.

15469-97-3

1-Tritylimidazole

1-Tritylimidazole is a potent inducer of cytochrome P450 enzymes, which play a critical role in drug metabolism and biotransformation. This compound enhances the enzymatic activity of various Cytochrome P450 isoforms, facilitating studies on drug interactions and metabolic pathways. Its applications extend to research in pharmacology, toxicology, and the development of therapeutic agents.

Cat. No.

A69846

CAS No.

98683-75-1

Ganolucidic acid B

Ganolucidic acid B is a triterpenoid compound that acts as an inducer of CYP3A4 via activation of human PXR (hPXR). This compound is significant in the study of metabolic pathways and drug metabolism, making it a valuable reagent for research into the regulation of cytochrome P450 enzymes. Ganolucidic acid B is useful for investigating the effects of metabolic inducers on pharmacokinetics and drug-drug interactions.

Cat. No.

A69900

CAS No.

72963-72-5

Imiprothrin

Imiprothrin is a potent inducer of CYP1A2, known for its significant effects on metallothionein 1a expression. This compound exhibits genotoxic and cytotoxic properties, evident through the initiation of detoxification responses in rat hepatocytes and the induction of chromosomal aberrations and micronucleus formation in bone marrow cells. Additionally, Imiprothrin prompts oxidative stress, resulting in lipid peroxidation and reactive oxygen species production, which can adversely affect liver and kidney functions. Though it inhibits weight gain and can lead to high mortality in female mice at elevated doses, it has not shown carcinogenicity in rat studies, with sensitive toxicity biomarkers including aspartate aminotransferase and total protein.

Cat. No.

A69951

CAS No.

20697-20-5

Methysticin

Synonyms: DL-Methysticin; (±)-Methystici

Methysticin is a kavalactone derived from kava extract, primarily acting as an inducer of CYP1A1. This compound is relevant in studies investigating metabolic enzyme modulation and its impact on drug metabolism. Additionally, it has potential implications in understanding the biochemical pathways associated with liver function and detoxification processes.