Cytochrome P450

Cat. No.

A69770

CAS No.

52601-58-8

CYP1B1-IN-7

CYP1B1-IN-7 is a selective inhibitor of the cytochrome P450 enzyme CYP1B1, exhibiting an IC50 value of 75 nM. This compound effectively reverses drug resistance in cancer cells, demonstrating an IC50 of 29 µM in the CYP1B1-overexpressing MCF-7 cell line resistant to Docetaxel. Its ability to induce cytotoxicity in resistant cell lines makes it a valuable tool for research on pharmacoresistance and the development of targeted cancer therapies.

Cat. No.

A69775

CAS No.

19993-32-9

Thermopsoside

Thermopsoside is a flavone derivative that functions as a specific inhibitor of CYP3A4. Demonstrating inhibitory effects on various CYP450 isozymes, it exhibits IC50 values of 6.0 μM for CYP3A4, alongside inhibitory activities against CYP2C19, CYP2D6, and CYP2C9 at concentrations of 9.5 μM, 12.0 μM, and 32.0 μM, respectively. This compound is valuable for research focused on drug metabolism and pharmacokinetics, particularly in studies exploring drug interactions mediated by CYP450 enzymes.

Cat. No.

A69777

CAS No.

786-97-0

SU 10603

SU 10603 is a specific inhibitor of cytochrome P45017A1 (CYP17A1). It effectively blocks the enzymatic activity responsible for the conversion of pregnenolone and progesterone into androgens, thereby regulating steroidogenesis. This compound is utilized in research applications related to hormone-driven conditions such as prostate cancer and adrenal hyperplasia, facilitating studies on the modulation of androgen levels.

Cat. No.

A69778

CAS No.

1174416-41-1

Dasatinib analog-1

Dasatinib analog-1 is a potent inhibitor of CYP3A4, achieving a Ki value of 5.4 μM. This compound effectively blocks the formation of glutathione adducts, making it valuable for studying drug metabolism and interactions. Its ability to modulate CYP3A4 activity positions it as a useful tool in pharmacological research and toxicology studies.

Cat. No.

A69780

CAS No.

62218-08-0

ε-Viniferin (epsilon-Viniferin)

Synonyms: epsilon-Viniferin

ε-Viniferin, a dimer of resveratrol, serves as a potent inhibitor of cytochrome P450 enzymes, exhibiting Ki values ranging from 0.5 to 20 μM. This compound is shown to possess significant antioxidant, anti-inflammatory, anti-diabetic, and anti-neurodegenerative properties. Its diverse biological activities make ε-Viniferin a valuable tool for research in pharmacology, toxicology, and disease models related to oxidative stress and inflammation.

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.

A69783

CAS No.

21535-97-7

3-Methylbenzofuran

3-Methylbenzofuran is a specific inhibitor of the cytochrome P450 enzyme CYP2A6, exhibiting an IC50 of 7.35 μM. This compound is particularly relevant for studies investigating tobacco-related carcinogenesis, providing insights into metabolic pathways involved in the activation of tobacco-derived carcinogens. Its role in modulating CYP2A6 activity makes it a valuable tool in chemical research focused on cancer biology and pharmacology.

Cat. No.

A69785

CAS No.

71140-51-7

(R)-Mephenytoin

Synonyms: (-)-Mephenytoin

(R)-Mephenytoin is the R-enantiomer of Mephenytoin, a compound that functions primarily as an anticonvulsant agent. It is utilized in research to investigate its effects on seizure control and its pharmacological properties. This enantiomer may also provide insights into the stereoselective metabolism and efficacy of anticonvulsant therapies.

Cat. No.

A69787

CAS No.

1438071-12-5

GSK2945

GSK2945 is a potent activator of cytochrome P450, specifically enhancing cholesterol 7α-hydroxylase (CYP7A1) activity. It demonstrates high specificity as a Rev-erbα antagonist, with EC50 values of 21.5 μM for mouse and 20.8 μM for human. This compound is primarily utilized in research focused on cholesterol metabolism and its regulatory mechanisms, offering insights into lipid homeostasis and related metabolic disorders.

Cat. No.

A69789

CAS No.

1356479-78-1

CYP11B2-IN-1

CYP11B2-IN-1 is a potent inhibitor of CYP11B2, exhibiting an IC50 of 2.3 nM. Additionally, it demonstrates inhibitory activity against CYP11B1 with an IC50 of 142 nM. This compound is primarily utilized in research focused on steroidogenesis, hypertension, and cardiovascular diseases. Its selective inhibition properties make it a valuable tool for studying adrenal enzymatic pathways and developing therapeutic strategies.

Cat. No.

A69790

CAS No.

1314116-53-4

Clopidogrel-β-D-glucuronide

Clopidogrel-β-D-glucuronide is an inhibitor of the CYP2C8 enzyme. As a metabolite of Clopidogrel, it selectively binds to CYP2C8, resulting in significant inhibition of this liver enzyme's activity. This compound plays a crucial role in understanding drug metabolism and interactions, making it valuable for research applications in pharmacology and toxicology.

Cat. No.

A69791

CAS No.

841-73-6

Bucolome

Synonyms: Paramidin; Paramidine

Bucolome is a selective inhibitor of cytochrome P450 2C9 (CYP2C9), primarily used for its uricosuric and anti-inflammatory properties. Its mechanism of action facilitates the increased excretion of uric acid, making it valuable in the research of hyperuricemia and related conditions. Bucolome's modulation of CYP2C9 activity also provides a useful tool for studying drug metabolism and interactions in pharmacological research.

Cat. No.

A69792

CAS No.

94356-22-6

Rhapontigenin 3'-O-glucoside

Rhapontigenin 3'-O-glucoside is a derivative of Rhapontigenin, functioning primarily as an inhibitor of cytochrome P450 enzymes, particularly human P450 1A1. This compound exhibits notable biological activity in modulating enzymatic pathways associated with drug metabolism and carcinogenesis. Its potential applications in cancer chemoprevention research make it a valuable reagent for studies examining the role of P450 enzymes in oncogenic processes.

Cat. No.

A69794

CAS No.

193079-69-5

Tabimorelin

Synonyms: NN703

Tabimorelin is a potent inhibitor of the CYP3A4 enzyme. This compound is recognized for its ability to act as an orally active growth hormone (GH) secretagogue, stimulating the release of GH in a physiological context. Its dual role as a CYP3A4 inhibitor has implications in drug metabolism studies and in understanding pharmacokinetic interactions. Tabimorelin is utilized in research related to endocrine function and therapeutic applications in conditions characterized by GH deficiency.

Cat. No.

A69795

CAS No.

119141-89-8

(R)-Esomeprazole

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.

Cat. No.

A69798

CAS No.

502656-68-0

CAY 10462 dihydrochloride

CAY 10462 dihydrochloride is a potent inhibitor of CYP4A hydroxylase. This compound enhances the contractile response to angiotensin II, demonstrating a maximal contractile response (Emax) at 6764 mg. CAY 10462 dihydrochloride is valuable for research focused on cardiovascular physiology and metabolic pathways involving cytochrome P450 enzymes.

Cat. No.

A69800

CAS No.

18110-87-7

4,5-Dimethoxycanthin-6-one

4,5-Dimethoxycanthin-6-one is a potent uncompetitive inhibitor of CYP1A2, exhibiting an IC50 value of 1.7 μM and a Ki value of 2.6 μM in phenacetin O-deethylation assays. This alkaloid, derived from the wood of Picrasma quassioides BENNET (Simaroubaceae), serves as a valuable tool for studying CYP1A2-mediated drug metabolism and interactions. Its inhibitory properties make it suitable for research applications in pharmacology and toxicology.

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.

A69803

CAS No.

112560-33-5

Keto-itraconazole

Synonyms: keto-ITZ

Keto-itraconazole, a potent inhibitor of CYP3A, is a metabolite of Itraconazole. It demonstrates a significant unbound IC50 value of 4.6 nM when assessed using human liver microsomes in conjunction with midazolam. This compound is valuable for research focused on drug metabolism and interactions involving CYP3A-mediated pathways.

Cat. No.

A69804

CAS No.

4430-31-3

Octahydrocoumarin

Octahydrocoumarin is a potent inhibitor of the cytochrome P450 enzyme CYP2A13, exhibiting an IC50 value of 6.6 μM. This compound's inhibition of CYP2A13 makes it a valuable tool for investigating drug metabolism and potential interactions in chemical research. It is particularly relevant for studies related to the metabolism of various xenobiotics and therapeutic agents.

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.

A69809

CAS No.

912291-11-3

CYP2A6-IN-2

CYP2A6-IN-2 is a selective inhibitor of the cytochrome P450 isoform CYP2A6. This compound is primarily utilized in research focused on elucidating the mechanisms underlying nicotine dependence and metabolism. Its inhibition of CYP2A6 may provide valuable insights into the pharmacological profiles of nicotine and other substrates metabolized by this enzyme, facilitating the development of therapeutic strategies for addiction and related disorders.

Cat. No.

A69810

CAS No.

2305-05-7

γ-Dodecanolactone

γ-Dodecanolactone acts as an inhibitor of the cytochrome P450 enzyme CYP1A2, demonstrating an IC50 value of 58 µM and a pIC50 value of 4.24. This γ-lactone compound is suitable for studies investigating the biological implications of CYP1A2 inhibition, particularly in the context of diseases associated with this enzyme. Researchers can utilize γ-Dodecanolactone to explore metabolic pathways and drug interactions involving CYP1A2.

Cat. No.

A69812

CAS No.

1375603-36-3

Seviteronel racemate

Synonyms: VT-464 (racemate)

Seviteronel racemate is a potent inhibitor of cytochrome P450 17A1 (CYP17), specifically targeting the lyase activity associated with this enzyme. With a low nanomolar IC50 value, it effectively disrupts steroidogenesis, making it valuable for research into conditions related to hormone regulation and hormonal therapies. This compound is suitable for studies focused on cancer biology, particularly in understanding the mechanisms underlying testosterone biosynthesis in prostate cancer.

Cat. No.

A69817

CAS No.

2280834-99-1

CYP4A11/CYP4F2-IN-2

CYP4A11/CYP4F2-IN-2 is a selective inhibitor of CYP4A11 and CYP4F2, exhibiting IC50 values of 120 nM and 220 nM, respectively. This compound effectively inhibits the production of 20-HETE in rat kidney models, demonstrating potential in research related to diabetic nephropathy and autosomal dominant polycystic kidney disease. Its oral bioavailability makes it a valuable tool for exploring the therapeutic effects of CYP4A11 and CYP4F2 inhibition in relevant biological conditions.