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Cytochrome P450 (CYP) inhibitors act on heme enzymes that oxidize drugs, steroids and other lipophilic compounds. The name comes from the 450 nm absorption peak of a carbon monoxide-bound pigment, described in liver microsomes in 1964. Hepatic enzymes such as CYP3A4, CYP2C9 and CYP1A2 metabolize a large share of drugs and many environmental chemicals. Other members synthesize steroid hormones, among them CYP17A1, which is required for androgen production. The P450 system can also convert chemicals into toxic or carcinogenic metabolites, which links it closely to toxicology. Abiraterone inhibits CYP17A1, while clarithromycin and itraconazole serve as CYP3A4 inhibitors in drug-interaction studies. Alizarin is listed for its inhibition of enzymes in the CYP1 family.
Naringenin is a flavanone, a type of flavonoid, that is considered to have a bioactive effect on human health as antioxidant, free radical scavenger, anti-inflammatory, carbohydrate metabolism promoter, and immune system modulator.
Synonyms: 1-Aminobenzotriazole
ABT (1-Aminobenzotriazole )is a suicide substrate for (CYP)cytochrome P-450 and chloroperoxidase.
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.
Mephenytoin is a CYP2C19 substrate. Anticonvulsant.
Synonyms: Resorufin methyl ether
Methoxyresorufin is a fluorometric substrate for cytochrome P450 linked enzymes.
Synonyms: SMT C1100; BMN 195; VOX-C1100
Ezutromid is a novel Small utrophin's translation modulator with EC50 of 0.4 uM .
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.
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.
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.
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.
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.
Synonyms: (R)-Omeprazole; (+)-Omeprazole
(R)-Esomeprazole is an orally active modulator of cytochrome P450 enzymes, specifically targeting CYP2C19, CYP3A4, and CYP2C9. This compound is instrumental in studying metabolic processes and drug interactions, particularly in the context of digestive system diseases. Its ability to influence metabolic pathways makes it a valuable tool in pharmacological research.
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.
Thienyldecyl Isothiocyanate serves as a cytochrome P450 modulator, demonstrating significant antiproliferative activity against cancer cells. This compound exerts its effects through the inhibition of cytochrome P450 enzymes and the induction of phase II detoxification enzymes, impacting xenobiotic metabolism. Thienyldecyl isothiocyanate is valuable for research in cancer biology and pharmacology, particularly in studies exploring enzyme modulation and its implications for drug metabolism and efficacy.
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