Cytochrome P450

Cat. No.

A68207

CAS No.

618094-85-2

Guanfu base A hydrochloride

Guanfu base A hydrochloride is a selective inhibitor of the CYP2D6 enzyme, demonstrating significant potential in the management of arrhythmia-related disorders. This alkaloid exhibits inhibitory effects across various species, including humans, primates, and canines. Its ability to modulate CYP2D6 activity may provide valuable insights and therapeutic applications in pharmacology and toxicology research.

Cat. No.

A69678

CAS No.

2231294-96-3

Opevesostat

Synonyms: MK-5684; ODM-208

Opevesostat is a selective inhibitor of CYP11A1, designed for oral administration. This compound demonstrates significant potential in the study of metastatic castration-resistant prostate cancer (mCRPC), supporting research into therapeutic approaches targeting steroidogenesis. Its specificity for CYP11A1 makes it a valuable tool in understanding the biochemical pathways involved in androgen synthesis and cancer progression.

Cat. No.

A69680

CAS No.

19431-84-6

Curcumenol

Synonyms: (+)-Curcumenol

Curcumenol is a potent inhibitor of CYP3A4, exhibiting an IC50 value of 12.6 μM. This bioactive compound, derived from Curcuma zedoaria, demonstrates neuroprotective, anti-inflammatory, anti-tumor, and hepatoprotective activities. In studies, Curcumenol suppresses Akt-mediated NF-κB activation and inhibits the p38 MAPK signaling pathway in LPS-stimulated BV-2 microglial cells, making it a valuable tool for research in neuroinflammation and cancer therapy.

Cat. No.

A69681

CAS No.

790676-40-3

(S)-(+)-N-3-Benzylnirvanol

Synonyms: (+)-N-3-Benzylnirvanol

(S)-(+)-N-3-Benzylnirvanol is a selective and competitive inhibitor of the cytochrome P450 isoform CYP2C19, exhibiting a Ki value of 250 nM. This compound displays low inhibition against other CYP isoforms, including CYP1A2, CYP2A6, CYP2C8, CYP2C9, CYP2D6, CYP2E1, and CYP3A4. It is primarily utilized in pharmacological research to study drug metabolism and drug-drug interactions involving CYP2C19.

Cat. No.

A69683

CAS No.

142128-57-2

Levoketoconazole

Synonyms: (-)-Ketoconazole; (-)-Ketoconazol; (-)-R 41400

Levoketoconazole is the 2S,4R enantiomer of ketoconazole, functioning primarily as a potent inhibitor of cortisol synthesis. By specifically inhibiting enzymes such as CYP11B1, CYP11A1, and CYP17A1, Levoketoconazole effectively reduces the production of cortisol and testosterone. This compound is particularly relevant for research applications focusing on endogenous Cushing’s syndrome and related endocrine disorders.

Cat. No.

A69685

CAS No.

1954681-29-8

LKY-047

LKY-047 is a selective reversible inhibitor of cytochrome P450 2J2 (CYP2J2), exhibiting an IC50 of 1.7 μM. This compound demonstrates high specificity, remaining inactive against other human cytochrome P450 isoforms, including CYPs 1A2, 2A6, 2B6, 2C8, 2C9, 2C19, 2D6, 2E1, and 3A. LKY-047 is utilized in research applications focused on understanding the role of CYP2J2 in drug metabolism and cardiovascular diseases.

Cat. No.

A69689

CAS No.

145414-76-2

6',7'-Dihydroxybergamottin

Synonyms: 6′,7′-DHB

6',7'-Dihydroxybergamottin (6′,7′-DHB) is a furanocoumarin that acts as a potent inhibitor of the cytochrome P450 enzyme CYP3A4. This compound is instrumental in studying drug metabolism and interactions, making it valuable for research in pharmacokinetics and toxicology. Its ability to modulate CYP3A4 activity has implications for understanding the effects of herbal supplements and dietary compounds on drug efficacy and safety.

Cat. No.

A69693

CAS No.

206052-02-0

MS-PPOH

MS-PPOH is a selective inhibitor of cytochrome P450 epoxygenases, primarily targeting CYP2C8 and CYP2C9 with IC50 values of 15 μM and 11 μM, respectively. This compound demonstrates key biological activity through the modulation of enzymatic metabolism pathways, making it valuable for research in pharmacology and toxicology. Additionally, MS-PPOH features an alkyne group, enabling its application in click chemistry via copper-catalyzed azide-alkyne cycloaddition (CuAAc) for tagging and labeling in various biochemical assays.

Cat. No.

A69695

CAS No.

1820940-17-7

Lorundrostat

Synonyms: MT-4129

Lorundrostat is a selective inhibitor of CYP11B2, targeting aldosterone synthase. This compound exhibits significant antihypertensive activity and is primarily utilized in research focused on the management of high blood pressure and related cardiovascular conditions. Its ability to modulate aldosterone levels makes it a valuable tool in studying endocrine and cardiovascular function.

Cat. No.

A69700

CAS No.

76530-44-4

Azamulin

Azamulin is an irreversible, highly selective inhibitor of human CYP3A4, effectively targeting this crucial cytochrome P450 enzyme. With IC50 values ranging from 0.03 to 0.24 μM, Azamulin exhibits potent CYP3A inhibition, making it a valuable tool in the study of drug metabolism and pharmacokinetics. Additionally, it holds potential for research in anti-infection therapies, providing insights into therapeutic strategies against infectious agents.

Cat. No.

A69701

CAS No.

56010-88-9

Fomepizole hydrochloride

Synonyms: 4-Methylpyrazole hydrochloride

Fomepizole hydrochloride is a potent inhibitor of cytochrome P450 enzyme CYP2E1. It functions as a competitive inhibitor of alcohol dehydrogenase, effectively preventing the metabolic conversion of methanol and ethylene glycol into harmful metabolites. This compound is primarily used in clinical settings as an antidote for poisoning due to methanol or ethylene glycol exposure, showcasing its significant biological activity in toxicology research.

Cat. No.

A69703

CAS No.

5853-29-2

Cephaeline dihydrochloride

Synonyms: (-)-Cephaeline dihydrochloride; NSC 32944

Cephaeline dihydrochloride is a selective inhibitor of cytochrome P450 2D6 (CYP2D6), exhibiting an IC50 of 121 μM. This compound is utilized in research focusing on drug metabolism and pharmacogenomics, providing insights into CYP2D6-mediated drug interactions and variations in drug efficacy. Its specificity for CYP2D6 makes it a valuable tool for studies investigating the role of this enzyme in pharmacological responses.

Cat. No.

A69706

CAS No.

93879-40-4

(±)-N-3-Benzylnirvanol

(±)-N-3-Benzylnirvanol acts as an inhibitor of the cytochrome P450 enzyme CYP2C19. This racemic mixture, comprised of both (+)-N-3-Benzylnirvanol and (-)-N-3-Benzylnirvanol, exhibits potent inhibitory activity with Ki values of 0.25 μM and 5.3 μM, respectively, for the respective enantiomers. It is valuable in pharmacological research aimed at understanding drug metabolism and potential drug-drug interactions involving CYP2C19.

Cat. No.

A69714

CAS No.

92321-29-4

2-Phenyl-2-(1-piperidinyl)propane

2-Phenyl-2-(1-piperidinyl)propane is a selective and reversible inhibitor of the human cytochrome P450 enzyme CYP2B6, displaying an IC50 value of 5.1 μM and a Ki of 5.6. In addition to its primary activity, this compound also moderately inhibits CYP2D6 and CYP3A, with IC50 values of 74 μM and 200 μM, respectively. This reagent is pertinent for research into drug metabolism and interactions involving CYP2B6 and other related P450 enzymes.

Cat. No.

A69719

CAS No.

2685779-55-7

CYP1B1-IN-4

CYP1B1-IN-4 is a selective CYP1B1 inhibitor, demonstrating a potent inhibitory activity with an IC50 value of 0.2 nM. This compound exhibits low cytotoxicity and maintains high stability in both human and rat liver microsomes, making it suitable for pharmacological studies. Its selectivity and stability position CYP1B1-IN-4 as a valuable tool for research into CYP1B1-related biological pathways and diseases.

Cat. No.

A69726

CAS No.

4846-19-9

N-Nornuciferine

N-Nornuciferine is an aporphine alkaloid derived from lotus leaves that selectively inhibits the cytochrome P450 enzyme CYP2D6, with an IC50 value of 3.76 μM and a Ki of 2.34 μM. This compound plays an important role in pharmacological research by modulating drug metabolism and interactions. Its potency as a CYP2D6 inhibitor makes it a valuable tool for studies investigating drug efficacy and toxicity related to cytochrome P450 enzymatic pathways.

Cat. No.

A69728

CAS No.

2126874-77-7

TP0472993

TP0472993 is a potent and orally active dual inhibitor of cytochrome P450 enzymes CYP4A11 and CYP4F2, exhibiting IC50 values of 140 nM and 40 nM, respectively. This compound is valuable for investigating the role of these enzymes in renal diseases, contributing to a deeper understanding of their biological functions and potential therapeutic implications. Its selective inhibition profile makes TP0472993 a useful tool for studying the pharmacological effects related to cytochrome P450-mediated pathways.

Cat. No.

A69731

CAS No.

937263-81-5

ONT-993

Synonyms: AR 00440993

ONT-993 is a hydroxylated metabolite that primarily inhibits the cytochrome P450 enzyme CYP2D6, with an IC50 value of 7.9 µM. Additionally, ONT-993 induces metabolism-dependent inactivation of CYP3A, characterized by a KI of 1.6 µM. This compound is useful in research applications focused on drug metabolism and pharmacokinetics, particularly regarding interactions involving CYP450 enzymes.

Cat. No.

A69733

CAS No.

2744168-51-0

CYP11A1-IN-1

CYP11A1-IN-1 is an inhibitor of cytochrome P450 11A1 (CYP11A1), exhibiting an IC50 range of 201-2000 nM. This compound is valuable for research focusing on steroid hormone synthesis and the role of androgens in diseases such as prostate cancer. It offers potential applications in studies related to androgen receptor-dependent pathways and their therapeutic implications.

Cat. No.

A69738

CAS No.

34993-56-1

1-Ethynylpyrene

1-Ethynylpyrene is a potent inhibitor of cytochrome P450 enzymes, specifically P450 1A1, 1A2, and 2B1, displaying IC50 values of 0.18, 0.32, and 0.04 μM, respectively. This compound also serves as a versatile click chemistry reagent, featuring an alkyne group that facilitates copper-catalyzed azide-alkyne cycloaddition (CuAAc) for bioconjugation applications. Its unique properties make it valuable for studies involving drug metabolism and chemical biology.

Cat. No.

A69741

CAS No.

877-43-0

2,6-Dimethylquinoline

2,6-Dimethylquinoline is a selective inhibitor of CYP1A2, exhibiting an IC50 of 3.3 µM. Additionally, it shows inhibitory activity towards CYP2B6 with an IC50 of 480 µM. This compound, derived from the roots of Peucedanum praeruptorum, serves as a valuable tool for research into drug metabolism and pharmacokinetics, particularly in studies exploring cytochrome P450 enzyme modulation.

Cat. No.

A69743

CAS No.

7437-55-0

8-Geranyloxypsoralen

8-Geranyloxypsoralen is a furanocoumarin that serves as a potent inhibitor of cytochrome P450 3A4 (CYP3A4), exhibiting an IC50 value of 3.93 μM. This compound is commonly utilized in research to explore drug metabolism and potential interactions involving CYP3A4, which plays a critical role in the biotransformation of numerous therapeutic agents. The inhibition of CYP3A4 by 8-Geranyloxypsoralen can facilitate the study of pharmacokinetics and enzyme regulation in cellular models.

Cat. No.

A69745

CAS No.

1260006-20-9

Lapiteronel

Synonyms: CFG920

Lapiteronel is a nonsteroidal, orally active inhibitor of CYP17 and CYP11B2, functioning as a reversible dual inhibitor. This compound exhibits significant biological activity in the modulation of steroid hormone synthesis, making it a valuable tool for research in metastatic castration-resistant prostate cancer. Its role in inhibiting critical enzymatic pathways positions Lapiteronel as a potential therapeutic agent in advancing cancer treatment studies.

Cat. No.

A69746

CAS No.

88511-35-7

1-(Isothiazol-3-yl)ethan-1-one

Synonyms: 1-(Isothiazol-3-yl)ethanone

1-(Isothiazol-3-yl)ethan-1-one is a selective inhibitor of CYP2E1, an enzyme involved in the metabolism of various xenobiotics and endogenous compounds. This compound has demonstrated potential in modulating pathways relevant to oxidative stress and inflammation. Its applications extend to research on conditions such as rheumatoid arthritis and sepsis, providing insights into therapeutic strategies targeting these diseases.

Cat. No.

A69748

CAS No.

486-28-2

Fraxinol

Fraxinol is a potent inhibitor of cytochrome P450 enzymes, primarily investigated for its role in drug metabolism and biotransformation. This compound, isolated from Lobelia chinensis, has demonstrated significant biological activity, making it relevant in studies focusing on pharmacokinetics and potential drug interactions. Fraxinol can be utilized in research aimed at understanding the metabolic pathways and toxicity profiles of various pharmaceuticals.