Cytochrome P450

Cat. No.

A64100

CAS No.

3043683-33-3

hCYP1B1-IN-2

hCYP1B1-IN-2 is a highly selective inhibitor of the human cytochrome P450 1B1 enzyme (hCYP1B1). It demonstrates remarkable potency in inhibiting hCYP1B1 activity, with an IC50 value of 0.040 nM, alongside a Ki value of 21.71 pM, indicating effective mixed inhibition. This compound also effectively disrupts aryl hydrocarbon receptor (AhR) transcription activities, making it a valuable tool for research applications focused on cancer and toxicology.

Cat. No.

A64108

CAS No.

2785358-47-4

CYP1B1-IN-10

CYP1B1-IN-10 is a potent and selective inhibitor of human cytochrome P450 1B1 (hCYP1B1), exhibiting an IC50 value of 0.11 μM. This compound plays a significant role in the investigation of hormone-dependent tumors, including breast and ovarian cancers. Its specificity makes it a valuable tool for studying the therapeutic potential in oncology 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.

A64119

CAS No.

70648-26-9

1,2,3,4,7,8-Hexachlorodibenzofuran

Synonyms: 1,2,3,4,7,8-HxCDF

1,2,3,4,7,8-Hexachlorodibenzofuran is a selective activator of the CYP1A1 and CYP1B1 enzymes. It induces the expression of these cytochrome P450 enzymes and aryl hydrocarbon receptor repressor (AhRR) in human peripheral blood lymphocytes. This compound also stimulates ethoxyresorufin-O-deethylase activity, achieving approximately 20% of the response observed with TCDD at a BMR20TCDD of 0.115-0.143 nM. Its ability to modulate these pathways makes it a valuable tool for studying biological responses to environmental pollutants and the mechanisms of xenobiotic metabolism.

Cat. No.

A64598

CAS No.

3023438-19-6

CypD-IN-4

CypD-IN-4 is a potent and selective inhibitor of cyclophilin D (CypD), exhibiting high affinity with an IC50 of 0.057 μM. This compound is valuable in researching various conditions related to oxidative stress, neurodegenerative diseases, liver dysfunction, aging processes, autophagy, and diabetes. CypD-IN-4 facilitates the exploration of CypD's role in these pathologies, providing insights into potential therapeutic strategies.

Cat. No.

A64599

CAS No.

2651994-75-9

CypD-IN-3

CypD-IN-3 is a potent and selective inhibitor of cyclophilin D (CypD), demonstrating high affinity with an IC50 value of 0.01 μM. This compound is valuable for studying a range of biological processes and diseases, including oxidative stress, neurodegenerative disorders, liver diseases, aging, autophagy, and diabetes. Its specificity towards CypD makes it an important tool for elucidating the role of this target in various cellular functions and pathological conditions.

Cat. No.

A64600

CAS No.

3023438-33-4

CypE-IN-1

CypE-IN-1 is a highly potent and selective inhibitor of cyclophilin E (CypE), exhibiting an IC50 of 0.013 μM and a Ki value of 0.072 μM. This compound is valuable for investigating the role of CypE in various pathological conditions, including oxidative stress, neurodegenerative diseases, liver disorders, aging processes, autophagy, and diabetes. Researchers can utilize CypE-IN-1 to explore therapeutic strategies targeting CypE-related pathways.

Cat. No.

A66036

CAS No.

2714485-49-9

Verapamil-d3 hydrochloride

Synonyms: (±)-Verapamil-d3 hydrochloride; CP-16533-1-d3 hydrochloride

Verapamil-d3 hydrochloride is a deuterium-labeled derivative of the calcium channel blocker, verapamil hydrochloride. It serves as a potent inhibitor of P-glycoprotein (P-gp) and CYP3A4, facilitating detailed pharmacological studies. This stable isotope is primarily utilized in research related to hypertension, cardiac arrhythmias, and angina, providing insight into drug metabolism and transport mechanisms in various biological systems.

Cat. No.

A67488

CAS No.

873327-59-4

AR-C141990

AR-C141990 functions as a dual inhibitor of CYP2C9 and CYP3A4, exhibiting IC50 values of 16 μM for both enzymes. This compound is recognized for its significant bioactivity, particularly as it inhibits the monocarboxylate transporter MCT1 with a Ki value of 4.8 nM. AR-C141990 is employed in research applications focused on drug metabolism and pharmacokinetics, as well as studies investigating interactions between drugs and metabolic pathways.

Cat. No.

A67533

CAS No.

128914-47-6

17-HETE

17-HETE is a metabolite of arachidonic acid produced via cytochrome P-450 pathways, comprising the 17R-HETE and 17S-HETE enantiomers. It acts as an allosteric activator of cytochrome P450 1B1 and an ATPase inhibitor, thereby playing a significant role in the induction of cardiac hypertrophy. This compound is valuable for research in cardiovascular biology and cytochrome P450 enzyme activity.

Cat. No.

A67552

CAS No.

183509-25-3

17(S)-HETE

17(S)-HETE is a metabolite of arachidonic acid produced via cytochrome P-450 pathways. This compound functions as an allosteric activator of cytochrome P450 1B1 and inhibits ATPase activity, which may contribute to the induction of cardiac hypertrophy. 17(S)-HETE is primarily utilized in research focusing on cardiovascular biology and cytochrome P450 enzyme functions.

Cat. No.

A68077

CAS No.

1394-48-5

Guanfu base A

Guanfu base A is a potent noncompetitive inhibitor of CYP2D6, with a Ki value of 1.20 μM in human liver microsomes and 0.37 μM for the recombinant form. This antiarrhythmic alkaloid, derived from Aconitum coreanum, also exhibits competitive inhibition of CYP2D in monkey and dog microsomes, with Ki values of 0.38 μM and 2.4 μM, respectively. In addition to its CYP2D6 inhibitory activity, Guanfu base A demonstrates the ability to inhibit HERG channel current, making it relevant for studies in drug metabolism and cardiac electrophysiology.

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.

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.

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.