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P450

Cytochromes P450 (CYPs) are a superfamily of enzymes containing heme as a cofactor that function as monooxygenases. In mammals, these proteins oxidize steroids, fatty acids, and xenobiotics, and are important for the clearance of various compounds, as well as for hormone synthesis and breakdown. In plants, these proteins are important for the biosynthesis of defensive compounds, fatty acids, and hormones.CYPs are, in general, the terminal oxidase enzymes in electron transfer chains, broadly categorized as P450-containing systems. The term "P450" is derived from the spectrophotometric peak at the wavelength of the absorption maximum of the enzyme (450 nm) when it is in the reduced state and complexed with carbon monoxide. Most CYPs require a protein partner to deliver one or more electrons to reduce the iron (and eventually molecular oxygen).

  • (S)-(+)-N-3-Benzylnirvanol
    T67926790676-40-3
    (S)-(+)-N-3-Benzylnirvanol (ZSN-76403) is a cytochrome P450 CYP2C19 inhibitor with an IC50 value of 0.179 µM that can be used to study HIV infection.
    • $169
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  • Salvianolic Acid C
    T3149115841-09-3
    Salvianolic Acid C is extracted from the root of Salvia miltiorrhiza, a perennial plant in the genus Salvia.
    • $36
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  • Gemfibrozil
    T141525812-30-0
    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).
    • $30
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  • Naringin
    T059510236-47-2
    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.
    • $35
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  • Vorozole
    T26322129731-10-8In house
    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.
    • $191
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  • Naringenin
    T2838480-41-1
    Naringenin (NSC-11855) is a flavanone that is considered to have a bioactive effect on human health as antioxidant, free radical scavenger, antiinflammatory, carbohydrate metabolism promoter, immunity system modulater. This substance has also been shown to repair DNA.
    • $50
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  • Tebuconazole
    T17022107534-96-3
    Tebuconazole is an agricultural azole fungicide. It can also inhibit CYP51 (IC50s: 0.9 and 1.3 μM for Candida albicans CYP51 and truncated Homo sapiens CYP51, respectively).
    • $50
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  • Inz-1
    T27617897776-15-7In house
    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.
    • $46
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  • Fenofibrate
    T114949562-28-9
    Fenofibrate (Lipanthyl) is a peroxisome proliferator receptor alpha agonist. Fenofibrate is a synthetic phenoxy-isobutyric acid derivate and prodrug with antihyperlipidemic activity.
    • $32
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  • Diflubenzuron
    T708835367-38-5
    Diflubenzuron (Larvakil) is a benzoyl-urea insecticide, found to be a potent inhibitor of melanosome synthesis in mouse melanoma cells. Diflubenzuron has also been shown to inhibit TCDD-induced CYP1A1 expression in HepG2 cells.
    • $30
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  • Amentoflavone
    T34171617-53-4
    Amentoflavone (3',8''-Biapigenin), as a potent inhibitor of CYP3A4 and CYP2C9, can interact with many other medications. CYP3A4 and CYP2C9 are proteins used for drug metabolism in the body. Amentoflavone also is an inhibitor of human cathepsin B. It has antimalarial activity in trials significant affinities towards the Delta-1, kappa opioid receptors (as an antagonist) and binds to benzodiazepine receptors. Amentoflavone may be a potential lead for a new type of anti-inflammatory agents having the dual inhibitory activity of group II phospholipase A2 and cyclooxygenase. Amentoflavone and quercetin differentially exerted suppression of PGE2 biosynthesis via downregulation of COX-2/iNOS expression.
    • $30
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  • Bergaptol
    T2S1434486-60-2
    1. Bergaptol (4-Hydroxybergapten) shows very good radical scavenging activity. 2. Bergaptol is a potent inhibitor of debenzylation activity of CYP3A4 enzyme.
    • $29
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  • 1-Aminobenzotriazole
    T59531614-12-6
    1-Aminobenzotriazole (ABT) (ABT) is a non-specific cytochrome P450 (CYP) inhibitor.
    • $41
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  • 1-Ethynylnaphthalene
    T742715727-65-8
    1-Ethynylnaphthalene is a selective inhibitor of cytochrome P450 IB1
    • $41
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  • Lofemizole
    T5005365571-68-8
    Lofemizole is an antagonist of CYP1A2.
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  • Guan-fu base A hydrochloride(1394-48-5 free base)
    T8182L618094-85-2
    Guan-fu base A hydrochloride is an antiarrhythmic alkaloid was isolated from Aconitum coreanum. Guanfu base A is hydrochloride a CYP2D6 inhibitor of human, monkey, and dog isoforms.
    • $133
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  • (-)-Vorozole
    T26322L132042-69-4In house
    (-)-Vorozole is an orally active non-steroidal aromatase inhibitor with potency and selectivity. (-)-Vorozole has demonstrated antitumor activity in in vivo experiments. (-)-Vorozole is used in the study of breast cancer.
    • $195
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  • CYP17-IN-1
    T109232093317-51-0In house
    CYP17-IN-1 is an effective oral inhibitor of CYP17 that can inhibit CYP17 in rats and humans with IC50 of 15.8 and 20.1 nM.
    • $117
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  • N-Nornuciferine hydrochloride(4846-19-9 free base)
    TQ0296L
    N-Nornuciferine hydrochloride(4846-19-9 free base) (N-Nornuciferine hydrochloride) is an aporphine alkaloid in lotus leaf, significantly inhibits CYP2D6 (IC50: 3.76 μM, Ki: 2.34 μM).
    • $133
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  • Ellagic Acid Dihydrate
    T9328133039-73-3
    Ellagic Acid Dihydrate inhibit the CYP1A1-dependent activation of benzo[a]pyrene.
    • $50
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  • Beta-Tetralone
    T0660530-93-8
    Beta-Tetralone (2-Tetralone) is a ketone derivative of tetralin.
    • $38
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  • CYP1B1-IN-5
    T73042176442-56-1
    CYP1B1-IN-5 is a selective and potent cytochrome P450 1B1 (CYP1B1) inhibitor with an IC50 of 4.7 nM.CYP1B1-IN-5 can be used for the study of metabolism-related diseases.
    • $195
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  • Enerisant HCl
    T704891152749-07-9In house
    Enerisant HCl is a novel potent and selective histamine H3 receptor antagonist, a substrate for P-gp, mediated by cytochrome P450 (CYP) and transporter proteins.
    • $195
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  • Harman hydrochloride
    T3158L21655-84-5
    Harman hydrochloride can directly induce CYP1A1 gene expression in an AhR-dependent manner and may represent a novel mechanism by which harman promotes mutagenicity, co-mutagenicity and carcinogenicity.
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  • 7-BFC
    T117521220001-53-6
    7-BFC (7-Benzyloxy-4-(trifluoromethyl)coumarin) is a coumarin-like fluorescent substrate that serves as a biomarker for cytochrome P 450 and can be used to study CYP isoforms and cytochrome P 450 metabolism.
    • $38
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  • Cecropin B acetate
    TP1313L
    Cecropin B acetate induces NF-κB activation and suppresses CYP3A29 by disrupting the association of the PXR/retinoid X receptor alpha (RXR-α) complex with DNA sequences. Cecropin B acetate exhibits strong antimicrobial activity.
    • $87
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  • AG 045572
    T22025263847-55-8
    AG 045572 is a potent GnRH receptor antagonist that inhibits the GnRH receptor in humans and rats with Ki values of 6.0 nM and 3.8 nM, respectively.AG 045572 is metabolized by CYP3A and inhibits testosterone.
    • $157
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  • Albaconazole
    T7725187949-02-6In house
    Albaconazole (W-0027) is a small molecule fungal cytochrome P450 family member 51 (fungal CYP51A1) inhibitor. It is used in the treatment of fungal infections, skin and musculoskeletal disorders, and can be used in the study of vulvovaginal candidiasis, Chagas disease and genitourinary disorders.
    • $350
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  • 2,3-dihydrothieno-Thiadiazole Carboxylate
    T22003152467-47-5
    2,3-dihydrothieno-Thiadiazole Carboxylate is a CYP450 (CYP2E1 and CYP2B4) inhibitor.
    • $50
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  • NP10679
    T734472914889-88-4In house
    NP10679 is an orally available, selective, brain-penetrating, potent, and pH-sensitive N-methyl-D-aspartate (NMDA) receptor inhibitor of the GluN2B subunit.NP10679 inhibits histamine H1, hERG channels, and CYP enzymes, and may be useful in the study of epilepsy and ischemic stroke.
    • $293 TargetMol
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  • Cholesterol 24-hydroxylase-IN-1
    T607961613480-70-8In house
    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.
    • $56
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  • CYP11B2-IN-1
    T109221356479-78-1In house
    CYP11B2-IN-1 is an effective and selective inhibitor of CYP11B2 with IC50s of 2.3 nM and 142 nM for CYP11B2 and CYP11B1.
    • $58
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  • K777
    T15641233277-99-1In house
    K777 is a potent, orally active and irreversible inhibitor of cysteine protease. K777 is a potent CYP3A4 inhibitor (IC50= 60 nM). K777 is also a selective CCR4 antagonist featuring the potent chemotaxis inhibition. K777 irreversibly inhibits Cruzain, which is the major cysteine protease of Trypansoma cruzi, and cathepsins B and L. K777 targets cathepsin-mediated cell entry and wxibits a broad-spectrum antiviral activity. K777 inhibits EBOV and SARS-CoV pseudovirus entry with IC50 values of 0.87 nM and 0.68 nM, respectively.
    • $2,039
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  • MS-PPOH
    T41291206052-02-0In house
    MS-PPOH is a potent and selective inhibitor of cytochrome P450 (CYP) epoxygenase. MS-PPOH inhibits CYP2C8 and CYP2C9 with IC50s of 15 and 11 µM, respectively
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  • Antihistamine-1
    T103351186430-60-3In house
    Antihistamine-1 is an H1-antihistamine (Ki: 6.9 nM) with acceptable blood-brain barrier penetration and also an inhibitor of CYP2D6 and hERG channel (IC50s: 5.4 and 0.8 μM).
    • $53
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  • Nampt activator-2
    T726172237268-90-3In house
    Nampt activator-2 is a NAMPT activator (EC50: 0.023 μM). Nampt activator-2 has an affinity for CYP2C9, 2D6, and 2C19 with affinity values of 0.060 μM, 0.41 μM, and 0.59 μM, respectively.Nampt activator-2 can be used in the study of atherosclerosis, obesity, type II diabetes, insulin resistance, and type I diabetes.
    • $84
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  • PF-4981517
    T215481390637-82-7In house
    PF-4981517 (CYP3cide) is a efficient, specific and time-dependent inhibitor of cytochrome P4503A4 (CYP3A4). The IC 50 values for CYP3A activity are 0.03 μM,17 μM, and 71 μM for CYP3A4, CYP3A5, and CYP3A7, respectively. PF-4981517 is able to be used to distinguish the contributions of CYP3A4 versus CYP3A5 on drug Metabolism.
    • $41
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  • Piperine
    T300294-62-2
    Piperine (Bioperine) , a alkaloid, has been used in trials studying the treatment of multiple myeloma and deglutition disorders.
    • $29
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  • Cobicistat
    T62461004316-88-4
    Cobicistat (GS-9350) is a carbamate and thiazole derivative that functions as a CYTOCHROME P450 CYP3A INHIBITOR to enhance the concentration of ANTI-HIV AGENTS, with which it is used in combination, for the treatment of HIV INFECTIONS.
    • $38
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  • Itraconazole
    T101184625-61-6
    Itraconazole (R51211) is a triazole antifungal agent that inhibits cytochrome P-450-dependent enzymes required for ERGOSTEROL synthesis.
    • $34
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  • Clarithromycin
    T143481103-11-9
    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.
    • $50
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  • Rhapontigenin
    T3776500-65-2
    Rhapontigenin (Protigenin) is a mechanism-based, selective inactivator of cytochrome P450 1A1 (IC50: 400 nM), an aryl hydrocarbon hydroxylase which activates polycyclic aromatic hydrocarbons that act as procarcinogens. Rhapontigenin is a natural analog of resveratrol with antioxidant and anti-cancer activity. At higher concentrations, rhapontigenin inhibits the proliferation of HL-60R and HepG2 cancer cell lines (IC50: 48 μM).
    • $51
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  • Memantine hydrochloride
    T144341100-52-1
    Memantine hydrochloride (Memantine HCl) is an AMANTADINE derivative that has some dopaminergic effects. Memantine hydrochloride has been proposed as an antiparkinson agent.
    • $42
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  • Cedrol
    T559477-53-2
    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)
    • $37
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  • Galangin
    T3668548-83-4
    Galangin (Norizalpinin) is an agonist/antagonist of the arylhydrocarbon receptor, and also shows inhibition of CYP1A1 activity.
    • $30
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  • Isavuconazole
    T2305241479-67-4
    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.
    • $31
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  • Germacrone
    T29456902-91-6
    Germacrone, a major active component found in Curcuma zedoaria oil product, shows anti-inflammatory, antiandrogenic, and antivirus activities. It also inhibits the proliferation of glioma cells by promoting apoptosis.
    • $41
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  • Apigenin
    T2175520-36-5
    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.
    • $45
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  • Galeterone
    T6509851983-85-2
    Galeterone (VN 124) is an orally bioavailable small-molecule androgen receptor modulator and CYP17 lyase inhibitor with potential antiandrogen activity. Galeterone exhibits three distinct mechanisms of action: 1) as an androgen receptor antagonist, 2) as a CYP17 lyase inhibitor and 3) by decreasing overall androgen receptor levels in prostate cancer tumors, all of which may result in a decrease in androgen-dependent growth signaling. Localized to the endoplasmic reticulum (ER), the cytochrome P450 enzyme CYP17 (P450C17 or CYP17A1) exhibits both 17alpha-hydroxylase and 17, 20-lyase activities, and plays a key role in the steroidogenic pathway that produces progestins, mineralocorticoids, glucocorticoids, androgens, and estrogens.
    • $52
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  • Stiripentol
    T449849763-96-4
    Stiripentol (BCX2600) (STP) is an anticonvulsant agent, which can inhibit N-demethylation of CLB to NCLB mediated by CYP3A4 (noncompetitively) and CYP2C19 (competitively) with Ki of 1.59/0.516 μM and IC50 of 1.58/3.29 μM, respectively.
    • $47
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