cytochrome p450

Hypericin (Cyclosan) is a natural anthraquinone compound, an extract of Hypericum perforatum, which inhibits PKC, MAO, dopamine-beta-hydroxylase, reverse transcriptase, telomerase, and CYP, etc. Hypericin exhibits antimicrobial, antiviral, antitumor, and antidepressant activities.

CYP11B2-IN-1 is an effective and selective inhibitor of CYP11B2 with IC₅₀s of 2.3 nM and 142 nM for CYP11B2 and CYP11B1.

Vorozole (R83842) is an orally active, potent, and selective nonsteroidal aromatase inhibitor.Vorozole exhibits antitumor activity in vivo and may be used in the study of breast cancer.

Inz-1 is an effective and fungal-selective inhibitor of mitochondrial cytochrome bc1 with IC₅₀s of 8.092 and 45.320 μM for yeast and human. Inz-1 reverses Fluconazole or other triazole antifungals' resistance in the pathogenic fungus Candida albicans.

MS-PPOH is a potent and selective inhibitor of cytochrome P450 (CYP) epoxygenase, specifically inhibiting CYP2C8 and CYP2C9 with IC₅₀ values of 15 and 11 µM, respectively.

Cholesterol 24-hydroxylase-IN-1 is an orally active, selective, and potent inhibitor of cholesterol 24-hydroxylase (CH24H or CYP46A1) that crosses the blood-brain barrier.Cholesterol 24-hydroxylase-IN-1 may be useful in the study of epilepsy-like neurological disorders. Cholesterol 24-hydroxylase-IN-1 is used to study epilepsy-like neurological diseases.

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.

Atazanavir (BMS-232632)(BMS-232632) is an highly effective HIV-1 protease inhibitor.

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

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.

Ketoconazole (R-41400) is an imidazole antifungal agent with broad-spectrum antifungal activity that primarily acts by inhibiting the biosynthesis of ergosterol in the fungal cell membrane. Ketoconazole inhibits the fungal cytochrome P450-dependent enzyme lanosterol 14α-demethylase (CYP51), thereby blocking the conversion of lanosterol to ergosterol. This leads to damage to the cell membrane structure and permeability, consequently inhibiting fungal growth and producing an antifungal effect. In addition, ketoconazole is a non-selective cytochrome P450 (CYP) inhibitor, specifically inhibiting drug-metabolizing enzymes such as human CYP3A4. In terms of endocrinology, ketoconazole also inhibits various enzymes involved in steroid synthesis (CYP17A1, CYP11A1).

Fomepizole (4-Methylpyrazole) is used as an antidote in confirmed or suspected methanol or ethylene glycol poisoning. Fomepizole(4-Methylpyrazole) is a competitive inhibitor of alcohol dehydrogenase, the enzyme that catalyzes the initial steps in the metabolism of ethylene glycol and methanol to their toxic metabolites.

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.

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

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

Fenofibrate (Lipanthyl) is a PPARα agonist (EC50=30 μM) and is selective. Fenofibrate also inhibits cytochrome P450 isoforms, such as CYP2C19, CYP2B6, CYP2C9, CYP2C8, and CYP3A4. Fenofibrate exhibits antihyperlipidemic activity.

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).

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.

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

Atovaquone (Atavaquone) is a hydroxynaphthoquinone that has antimicrobial activity and is being used in antimalarial protocols.

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.

Doxepin hydrochloride (Aponal) is a dibenzoxepin tricyclic compound. It displays a range of pharmacological actions including maintaining adrenergic innervation. Its mechanism of action is not fully understood, but it appears to block reuptake of monoaminergic neurotransmitters into presynaptic terminals. It also possesses anticholinergic activity and modulates antagonism of histamine H(1)- and H(2)-receptors.

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.

Clobetasol propionate (CGP9555) exerts its effect by binding to cytoplasmic glucocorticoid receptors and subsequently activates glucocorticoid receptor-mediated gene expression. This results in the synthesis of certain anti-inflammatory proteins while inhibiting the synthesis of certain inflammatory mediators. Clobetasol Propionate is the propionate salt form of clobetasol, a topical synthetic corticosteroid with anti-inflammatory, antipruritic, and vasoconstrictive properties. Specifically, clobetasol propionate appears to induce phospholipase A2 inhibitory proteins, thereby controlling the release of the inflammatory precursor arachidonic acid from membrane phospholipids by phospholipase A2.