Cytochrome P450

Cat. No.

A46808

CAS No.

134-90-7

L-(+)-threo-Chloramphenicol

Synonyms: (+)-Chloramphenicol; Dextramycine; Dextromycetin

L-(+)-threo-Chloramphenicol is the S,S-stereoisomer of chloramphenicol, functioning primarily as an inhibitor of protein synthesis in reticulocytes. This compound also demonstrates inhibitory effects on the oxidative activity of isolated mitochondria. L-(+)-threo-Chloramphenicol is valuable for research applications in studying protein synthesis mechanisms and mitochondrial function.

Cat. No.

A47733

CAS No.

2751-09-9

Troleandomycin

Synonyms: Triacetyloleandomycin

Troleandomycin, a macrolide antibiotic, functions as a selective inhibitor of the cytochrome P450 enzyme CYP3A. This compound is primarily used in research to investigate drug metabolism and interactions related to CYP3A. Additionally, it has applications in studies involving corticosteroids for conditions such as asthma, providing insights into therapeutic efficacy and safety profiles.

Cat. No.

A48594

CAS No.

38210-27-4

Frutinone A

Frutinone A is a selective inhibitor of CYP1A2, featuring a chromonocoumarin structural scaffold. This compound exhibits notable antibacterial and antioxidant activities, making it a valuable tool for research in pharmacology and toxicology. Its ability to modulate the activity of CYP1A2 underscores its potential for studying drug metabolism and interactions.

Cat. No.

A49947

CAS No.

3065926-17-9

CYP1A1-IN-1

CYP1A1-IN-1 is a selective inhibitor of cytochrome P4501A1 (CYP1A1). This compound has demonstrated the ability to reduce bacterial loads of methicillin-resistant Staphylococcus aureus (MRSA) and Acinetobacter baumannii through the enhancement of macrophage phagocytosis. CYP1A1-IN-1 holds potential for advancing research in sepsis associated with multidrug-resistant (MDR) bacterial infections.

Cat. No.

A51010

CAS No.

161796-77-6

(R)-Omeprazole sodium

(R)-Omeprazole sodium is a cytochrome P450 inhibitor primarily targeting CYP2C19. This compound effectively inhibits gastric acid secretion and demonstrates reversible direct and metabolism-dependent inhibition of metabolic pathways influenced by cytochrome P450 enzymes. (R)-Omeprazole sodium's pharmacokinetics can be modified by interactions with excipients such as mannitol, potentially affecting its bioavailability in various formulations. Its applications include studies on gastric acid regulation and drug metabolism in pharmacological research.

Cat. No.

A51946

CAS No.

101236-49-1

Kushenol K

Kushenol K is a flavonoid antioxidant derived from the roots of Sophora flavescens, functioning as a selective inhibitor of cytochrome P450 3A4 (CYP3A4) with a Ki value of 1.35 μM. This compound exhibits weak antiviral activity against herpes simplex virus type 2 (HSV-2) with an EC50 of 147 μM. Additionally, Kushenol K inhibits sodium-glucose co-transporters SGLT1 and SGLT2, making it relevant for research in metabolic disorders and viral infections.

Cat. No.

A52219

CAS No.

110025-28-0

(E/Z)-Endoxifen

Endoxifen is an active metabolite of tamoxifen that primarily targets and modulates the estrogen receptor, exhibiting higher binding affinity and specificity. In addition, it functions as a cytochrome P450 inhibitor, effectively inhibiting aromatase activity. Due to its unique profile, Endoxifen is valuable for research applications in breast cancer biology and therapeutic development.

Cat. No.

A52241

CAS No.

1197194-41-4

Endoxifen hydrochloride

Endoxifen hydrochloride, a selective antagonist of estrogen receptors, serves as a significant active metabolite of Tamoxifen, exhibiting enhanced affinity and specificity. In addition to its receptor activity, Endoxifen hydrochloride also functions as a cytochrome P450 inhibitor, effectively inhibiting aromatase activity. This compound is utilized in breast cancer research, facilitating studies on therapeutic efficacy and mechanisms of action in estrogen-dependent tumors.

Cat. No.

A52244

CAS No.

16910-32-0

Obtusifoliol

Obtusifoliol is a selective inhibitor of cytochrome P450 51 (CYP51), demonstrating affinities with dissociation constants (Kd) of 1.2 μM for Trypanosoma brucei and 1.4 μM for human CYP51. This compound is significant in studies focused on trypanosomiasis, targeting the sterol biosynthesis pathway. Its inhibition of CYP51 may provide valuable insights into therapeutic strategies against related infections and contribute to the understanding of cholesterol metabolism in various biological systems.

Cat. No.

A52457

CAS No.

1361414-26-7

SR9186

Synonyms: ML368

SR9186 is a selective inhibitor of CYP3A4, demonstrating potent inhibition with IC50 values of 9 nM for the metabolism of Midazolam, 4 nM for Testosterone, and 38 nM for Vincristine. This compound effectively impedes hepatic-stage P. falciparum development and obstructs the metabolism of ivermectin. Its utility extends to breast cancer research, making it a valuable tool for investigating drug metabolism and therapeutic applications.

Cat. No.

A52903

CAS No.

1246770-52-4

VNI

VNI is a potent inhibitor of cytochrome P450 51 (CYP51), targeting sterol synthesis in the parasite Trypanosoma cruzi. Its mechanism of action disrupts the biosynthesis of essential sterols, leading to impaired growth and viability of the pathogen. VNI is primarily utilized in research focused on anti-parasitic strategies and the development of therapeutics for Chagas disease.

Cat. No.

A52911

CAS No.

3034186-60-9

CYP51-IN-15

CYP51-IN-15 is a selective inhibitor of CYP51, targeting the enzyme in Naegleria fowleri. With an EC50 value of 1.5 μM, it demonstrates potent biological activity against this pathogenic organism. This compound is valuable in research aimed at elucidating mechanisms of action and developing therapeutic strategies against Naegleria fowleri infections.

Cat. No.

A52987

CAS No.

327042-42-2

LP8

LP8 is a pyridinyl-type inhibitor of cytochrome P450 51 (CYP51), specifically targeting the sterol biosynthesis pathway in various pathogens. This compound exhibits significant biological activity against Trypanosoma cruzi, the causative agent of Chagas disease and American trypanosomiasis. LP8 is valuable for research applications aimed at elucidating the mechanisms of these diseases and developing potential therapeutic strategies.

Cat. No.

A53006

CAS No.

1033846-45-5

SDZ-285604

Synonyms: VNF

SDZ-285604 is a specific inhibitor of sterol 14-demethylase (CYP51) in Trypanosoma cruzi. This compound demonstrates potent activity against the enzyme, making it a valuable tool for investigating the pathogenesis of Chagas disease. Research applications include studying the biochemical pathways involved in T. cruzi infection and exploring potential therapeutic strategies.

Cat. No.

A53585

CAS No.

3010895-54-9

CYP2C1/CYP2C19-IN-2

CYP2C1/CYP2C19-IN-2 is a potent inhibitor of the CYP2C1 and CYP2C19 enzymes. This compound exhibits minimal hepatotoxicity and lacks Ames toxicity, making it a safer choice for research applications. CYP2C1/CYP2C19-IN-2 is particularly useful in studies investigating antiviral mechanisms against Zika virus (ZIKV).

Cat. No.

A53609

CAS No.

3010895-55-0

CYP2C9/CYP2C19-IN-1

CYP2C9/CYP2C19-IN-1 is a potent inhibitor of the cytochrome P450 enzymes CYP2C9 and CYP2C19. This compound exhibits key biological activity by effectively modulating drug metabolism pathways without hepatotoxic effects or Ames toxicity. It serves as a valuable tool for research applications, including studies on anti-Zika virus (ZIKV) therapeutics.

Cat. No.

A53769

CAS No.

173026-17-0

ALT-2074

Synonyms: BXT-51072

ALT-2074 is a CYP3A inhibitor with an IC50 value ranging from 2.0 to 2.6 μM, functioning as a catalytic analogue of glutathione peroxidase. Although it demonstrates a weak inhibitory effect on CYP3A in vivo, it serves as a valuable tool for studying the role of oxidative stress in inflammatory diseases, including acute coronary syndrome. This compound is particularly useful in research investigating the interplay between reactive oxygen species and metabolic pathways.

Cat. No.

A57006

CAS No.

1572646-93-5

CypD-IN-5

CypD-IN-5 is a selective inhibitor of cyclophilin D (CypD), a key regulator of mitochondrial permeability transition. This compound demonstrates significant potential in modulating mitochondrial function and may be particularly useful in studying neurodegenerative diseases such as Alzheimer's disease. Its application in research focuses on understanding the role of CypD in cellular stress responses and the underlying mechanisms of neurodegeneration.

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.

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.

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.

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.