Cytochrome P450

Cat. No.

A10081

CAS No.

520-36-5

Apigenin

Synonyms: 4',5,7-Trihydroxyflavone; Apigenol; C.I. Natural Yellow 1

Apigenin, found in many plants, is a natural product belonging to the flavone class that is the aglycone of several naturally-occurring glycosides. Apigenin acts as a monoamine transporter activator, one of the few chemicals demonstrated to possess this property. Apigenin is a ligand for central benzodiazepine receptors that competitively inhibited the binding of flunitrazepam with a Ki of 4μM, exerting anxiolytic and slight sedative effects.

Cat. No.

A19393

CAS No.

88678-67-5

Pyributicarb

Synonyms: TSH-888

Pyributicarb, a carbamate-type herbicide, is a potent activator of both CYP3A4 gene and human pregnane X receptor (hPXR).

Cat. No.

A21011

CAS No.

1093130-72-3

Veledimex

Synonyms: INXN-1001; RG-115932

Veledimex is an oral activator ligand for a proprietary gene therapy promoter system, and a moderate inhibitor of and substrate for CYP3A4/5.

Cat. No.

A46361

CAS No.

480-66-0

Phloracetophenone

Synonyms: 2,4,6-trihydroxyacetophenone; 1-(2,4,6-Trihydroxyphenyl)ethanone

Phloracetophenone is a cytochrome P450 activator that primarily enhances the activity of cholesterol 7α-hydroxylase (CYP7A1). This compound exhibits cholesterol-lowering properties, making it a valuable tool for research into lipid metabolism and cholesterol regulation. Additionally, Phloracetophenone stimulates bile secretion through the mediation of Mrp2, further supporting its role in studies focused on liver function and gallbladder health.

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.

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.

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.

A69950

CAS No.

73804-65-6

11-HETE

Synonyms: 11-Hydroxy-5,8,12,14-eicosatetraenoic acid

11-HETE (11-Hydroxy-5,8,12,14-eicosatetraenoic acid) serves as an activator for cytochrome P450 enzymes. This compound is known to upregulate the mRNA expressions of CYP1B1, CYP1A1, CYP4A11, CYP4F11, and CYP4F2, leading to significant biological effects such as cell hypertrophy in RL-14 cells. Due to its modulatory role in cytochrome P450 activity, 11-HETE holds potential applications in the study of cardiovascular diseases.