p450

Cytochrome P450 2C9 is a cytochrome P-450 subtype that possesses specificity for acidic xenobiotics. It oxidizes a wide range of important clinical drugs under the categories of nonsteroidal anti-inflammatory agents, anticoagulants, hypoglycemic agents, a

Cytochrome P450 CYP1B1 (190-198) [Homo sapiens] is a peptide from Cytochrome c, which is a small heme protein found loosely associated with the inner membrane of the mitochondrion. Cytochromes c from certain eukaryotes, including plants and fungi but not higher animals, contains methylated lysine residues at specific positions1. Cytochrome c is a required cofactor for Apaf-1 function2.

Cytochrome P450 reductase, a NADPH-cytochrome reductase, facilitates an optimal conformation of aromatase for substrate binding [1].

(S)-(+)-N-3-Benzylnirvanol (ZSN-76403) is a cytochrome P450 CYP2C19 inhibitor with an IC50 of 0.179 µM, suitable for studying HIV infection.

Salvianolic Acid C is extracted from the root of Salvia miltiorrhiza, a perennial plant in the genus Salvia.

1. Hypericin (Cyclosan) has antineoplastic activity. 2. Hypericin has antibiotic and antiviral activities. 3. Hypericin has antidepressive activity through inhibiting monoamine oxidase enzyme. 4. Hypericin inhibits RANKL-mediated osteoclastogenesis via affecting ERK signalling in vitro and suppresses wear particle-induced osteolysis in vivo.

Bifonazole (Bay H-4502) acts to destabilize the fungal cytochrome p450 51 enzyme (also known as Lanosterol 14-alpha-demethylase). It works by inhibiting the production of a substance called ergosterol, which is an essential component of fungal cell membranes. This is vital in the cell membrane structure of the fungus. Its inhibition leads to cell lysis. The disruption in production of ergosterol disrupts the cell membrane and causes holes to appear. The cell membranes of fungi are vital for their survival. They keep unwanted substances from entering the cells and stop the contents of the cells from leaking out.

Isonicotinic acid, a metabolite of isoniazid and a useful isomer of nicotinic acid, is formed from isoniazid by hydrazinolysis and can be catalyzed by cytochrome P450 enzymes, such as CYP2C.

Itraconazole (R51211) is a triazole antifungal agent that inhibits cytochrome P-450-dependent enzymes necessary for ERGOSTEROL synthesis.

Gemfibrozil (CI-719) interacts with peroxisome proliferator-activated receptors (PPARalpha) resulting in PPARalpha-mediated stimulation of fatty acid oxidation and an increase in lipoprotein lipase (LPL) synthesis. Gemfibrozil is a fibric acid derivative with hypolipidemic effects. This enhances triglyceride-rich lipoprotein clearance and reduces the expression of apolipoprotein C-III (apoC-III). The reduction in hepatic production of apoC-III result in the subsequent reduction of serum levels of very-low-density-lipoprotein cholesterol (VLDL-C). In addition, gemfibrozil-mediated PPARalpha stimulation of apoA-I and apoA-II expression results in an increase in high-density lipoprotein cholesterol (HDL-C).

2-Benzothiazolamine (2-ABT) is a nitrogen-containing heterocyclic compound used as a reaction intermediate in the synthesis of a variety of drugs. It inhibits cytochrome P450 activity and has also shown anti-inflammatory, anticonvulsant and anticancer activities in animal models.

Clarithromycin (A-56268) is a Macrolide Antimicrobial. The mechanism of action of clarithromycin is as a Cytochrome P450 3A4 Inhibitor, and Cytochrome P450 3A Inhibitor, and P-Glycoprotein Inhibitor. The chemical classification of clarithromycin is Macrolides.

7-Ethoxycoumarin, a typical human P450 substrate, is catalyzed by both wild-type and mutant forms of CYP102A1.

Memantine hydrochloride (Memantine HCl) is an AMANTADINE derivative that has some dopaminergic effects. Memantine hydrochloride has been proposed as an antiparkinson agent.

Cedrol is a cedrane sesquiterpenoid and a tertiary alcohol,Cedrol inhibits the cytochrome P450 (CYP) isoforms CYP2B6 and CYP3A4 (Kis = 0.9 and 3.4 μM, respectively)

Galangin (Norizalpinin) is an agonist antagonist of the arylhydrocarbon receptor, and also shows inhibition of CYP1A1 activity.

Hexaconazole ((-)-Hexaconazol) is a broad-spectrum triazole fungicide that inhibits ergosterol biosynthesis via inhibition of the cytochrome P450-dependent 14α-demethylation of lanosterol, which results in disruption of the fungal cell membrane and cell death.

Isavuconazole (RO-0094815)(BAL-4815; RO-0094815) is the active component of the new azole antifungal agent BAL8557 with MIC(50)s/MIC(90)s ranged from 0.002/0.004 mg/liter for C. albicans to 0.25/0.5 mg/liter for C. glabrata.

Apigenin (NSC 83244) is an aromatic oil extracted from the flowers or leaves of the daisy-like plants. Extracts, oils and teas made from chamomile are used for its soothing qualities as a sedative, mild analgesic and sleep medication. Apigenin has not been implicated in causing serum enzyme elevations or clinically apparent liver injury.

Voriconazole (UK-109496) is a triazole antifungal agent that specifically inhibits STEROL 14-ALPHA-DEMETHYLASE and CYTOCHROME P-450 [CYP3A].

Abiraterone Acetate (CB7630) is an androstene derivative that inhibits STEROID 17-ALPHA-HYDROXYLASE and is used as an ANTINEOPLASTIC AGENT in the treatment of metastatic castration-resistant PROSTATE CANCER.

Clomethiazole (Distraneurin) is an orally active GABAA agonist and it is an anticonvulsant agent. It also has the potential for treating convulsive status epilepticus. Chlormethiazole inhibits cytochrome P450 isoforms: CYP2A6 and CYP2E1 in human liver microsomes.

2-Naphthol is a metabolite of naphthalene, catalyzed by cytochrome P450 isoforms (CYP 1A1, CYP 1A2, CYP 2A1, CYP 2E1, and CYP 2F2). 2-Naphthol is cytotoxic.

Naringin (Naringoside), a flavanone glycoside, exerts various of pharmacological effects such as blood lipid lowering, antioxidant activity, anticancer activity, and inhibition of cytochrome P450 enzymes.

Abiraterone (CB-7598) (CB-7598) is an effective steroidal cytochrome P450 17alpha-hydroxylase-17, 20-lyase (CYP17) inhibitor (IC50: 4 nM).

Flavone (2-Phenyl-4-chromone) have effects on CYP (P450) activity which are enzymes that metabolize most drugs in the body.

Clotrimazole (FB 5097), an imidazole derivative with a broad spectrum of antimycotic activity, inhibits biosynthesis of the sterol ergostol.

Sulfamethoxazole (STX 608) is a Sulfonamide Antimicrobial. The mechanism of action of sulfamethoxazole is as a Cytochrome P450 2C9 Inhibitor. The chemical classification of sulfamethoxazole is Sulfonamides.

Verapamil hydrochloride (Verapamil HCl) is a calcium channel blocker that is a class IV anti-arrhythmia agent.

Quinidine sulfate dihydrate (Pitayine Sodium) is a potent and selective cytochrome P450db inhibitor

Chlorzoxazone (Chlorzoxazon) is a Muscle Relaxant. The physiologic effect of chlorzoxazone is by means of Centrally-mediated Muscle Relaxation.

Efavirenz (DMP 266) is a Human Immunodeficiency Virus 1 Non-Nucleoside Analog Reverse Transcriptase Inhibitor, acting as a Non-Nucleoside Reverse Transcriptase Inhibitor, Cytochrome P450 3A Inducer, Cytochrome P450 2B6 Inducer, Cytochrome P450 2C9 Inhibitor, Cytochrome P450 2C19 Inhibitor, and Cytochrome P450 3A4 Inhibitor, classified as a Non-Nucleoside Analog.

Climbazole (BAY-e 6975) is a broad-spectrum imidazole antifungal agent with anti-dandruff properties.

Methoxsalen (NCI-C55903) is a Photoactivated Radical Generator and Psoralen. The mechanism of action of methoxsalen is as a Photoabsorption. The physiologic effect of methoxsalen is by means of Photosensitizing Activity.

Clopidogrel hydrogen sulfate ((S)-(+)-Clopidogrel bisulfate) , a selective, high-affinity P2Y12 receptor antagonist, suppressess fibrinogen binding to platelets and platelet adhesion and aggregation.

Alizarin (Mordant Red 11), a red dye derived from the roots of plants of the madder genus, inhibits P450 isoform CYP1A1( IC50 = 6.2 μM), CYP1A2 (IC50 =10.0 μM )and CYP1B1(IC50 = 2.7 μM).

Atazanavir sulfate (BMS-232632 sulfate) is an azapeptide and HIV-protease inhibitor used in the treatment of HIV infections and AIDS in combination with other anti-HIV agents.

6-Hydroxyflavone (6-HF) is a noncompetitive inhibitors of cytochrome P450 2C9. It is a flavone, a type of chemical compound. It is reported in leaves of Barleria prionitis Linn. (a common Acanthaceae from India). 6-Hydroxyflavone may have a potential as a therapeutic drug capable for the treatment of anxiety-like disorders.

Ranitidine Hydrochloride (AH19065) is a member of the class of histamine H2-receptor antagonists with antacid activity. Ranitidine is a competitive and reversible inhibitor of the action of histamine, released by enterochromaffin-like (ECL) cells, at the histamine H2-receptors on parietal cells in the stomach, thereby inhibiting the normal and meal-stimulated secretion of stomach acid. In addition, other substances that promote acid secretion have a reduced effect on parietal cells when the H2 receptors are blocked.

Bergapten (5-Methoxypsoralen), a psoralen, inhibits cell replication.

Trimethoprim (NSC-106568) is a Dihydrofolate Reductase Inhibitor Antibacterial. The mechanism of action of trimethoprim is as a Dihydrofolate Reductase Inhibitor, and Cytochrome P450 2C8 Inhibitor, and Organic Cation Transporter 2 Inhibitor.

1-Ethynylnaphthalene [1-EN] is a selective inhibitor of cytochrome P450 IB1 (CYP1B1).

Quinidine is a stereoisomer of the antimalarial agent quinine and a class Ia antiarrhythmic agent. for the treatment of abnormal heart rhythms and also malaria.

3-Chloropropiophenone (CPP) is a synthetic compound that is used in the synthesis of organic reagents, pharmaceuticals, and other products. It has the ability to inhibit certain enzymes (e.g. cytochrome P450) and inhibit the growth of certain tumor cells.

Pitavastatin calcium (NK-104) is a potent inhibitor of HMG-CoA reductase (Ki: 1.7 nM). It lowers both total cholesterol and low-density lipoprotein cholesterol in animals and humans. Metabolism of pitavastatin by the cytochrome P450 system is minimal, reducing the risk of drug-drug interactions.

Piperonylic acid (2H-1,3-benzodioxole-5-carboxylic acid) is a natural molecule bearing a methylenedioxy function that closely mimics the structure of trans-cinnamic acid. Piperonylic acid selectively inactivate the CYP73A P450 subpopulation.

Diosmetin (Luteolin 4-methyl ether) has been found to act as a weak TrkB receptor agonist.

1-Aminobenzotriazole (ABT) (ABT) is a non-specific cytochrome P450 (CYP) inhibitor.

Aprepitant (Aprepitant`) is a Substance P/Neurokinin-1 Receptor Antagonist. The mechanism of action of aprepitant is as a Neurokinin 1 Antagonist, and Cytochrome P450 3A4 Inhibitor, and Cytochrome P450 2C9 Inducer, and Cytochrome P450 3A4 Inducer.

Uniconazole is a plant growth regulator that inhibit cytochrome P450 707As (Ki=68 nM). CYP707As is a major ABA catabolic enzyme that catabolize Abscisic acid, accordingly suppress gibberellin and sterol biosynthesis.