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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).

  • Opevesostat
    T776272231294-96-3
    Opevesostat (ODM-208) is an inhibitor of lyase (CYP11A1) (the enzyme cleavage cholesterol side chain).
    • $30
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  • (S)-(+)-N-3-Benzylnirvanol
    T67926790676-40-3
    (S)-(+)-N-3-Benzylnirvanol is a cytochrome P450 CYP2C19 inhibitor with a ki value of 82.5μM for CYP2C9 and 0.25μM for CYP2C19, which can be used to study HIV infection.
    • $147
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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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  • 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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  • Dihydromethysticin
    TQ019119902-91-1
    Dihydromethysticin ((+)-Dihydromethysticin) is a kavalactone found in Piper methysticum. It has marked activity on the induction of CYP3A23.
    • $70
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  • Tauroursodeoxycholate
    T253214605-22-2
    Tauroursodeoxycholate (UR 906), also known as ursodoxicoltaurine, is a highly hydrophilic tertiary bile acid that is produced in humans at a low concentration. Tauroursodeoxycholate is the more hydrophilic form of ursodeoxycholic acid, which is the more abundant naturally produced bile acid in humans.Tauroursodeoxycholate is being investigated for use in several conditions such as Primary Biliary Cirrhosis (PBC), insulin resistance, amyloidosis, Cystic Fibrosis, Cholestasis, and Amyotrophic Lateral Sclerosis.
    • $50
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  • Glycycoumarin
    TN170294805-82-0
    Glycycoumarin is an estrogen agonist, it shows moderate inhibitory effects against CYP1A2 and CYP2B6.
    • $74
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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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  • Ginsenoside C-K
    T381139262-14-1
    Ginsenoside C-K (Ginsenoside K) is a bacterial metabolite of G-Rb1 exhibiting anti-inflammatory effects by reducing iNOS and COX-2.
    • $110
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  • Soticlestat
    T89371429505-03-2
    Soticlestat (OV935) is a potent, selective and orally active cholesterol 24-hydroxylase (CYP46A1) inhibitor. It has the potential for epilepsy syndromes research.
    • $60
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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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  • Avasimibe
    T2753166518-60-1
    Avasimibe (PD-148515) is an orally bioavailable inhibitor of acyl-Coenzyme A: cholesterol acyltransferase (ACAT, IC50: 3.3 μM) that prevents cholesterol deposition in the arterial wall. It also inhibits human P450 isoenzymes CYP2C9 1A2 2C19 (IC50: 2.9 13.9 26.5 μM).
    • $43
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  • Verapamil
    T2065652-53-9
    Verapamil (CP-16533-1) is a calcium channel blocker and an orally active and effective inhibitor of P-gp. Verapamil inhibits CYP3A4 and can be used in studies about the treatment of high blood pressure, heart arrhythmias, and angina research.
    • $30
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  • Glabrol
    TN169159870-65-4
    5-Methylcytosine is a methylated nucleotide base found in eukaryotic DNA. It is an epigenetic modification formed by the action of DNA methyltransferases.
    • $73
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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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  • Miltirone
    TN102327210-57-7
    Miltirone is a CYPs inhibitor, it has been characterized as a low-affinity ligand for central benzodiazepine receptors.
    • $135
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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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  • Abiraterone
    T6216154229-19-3
    Abiraterone (CB-7598) (CB-7598) is an effective steroidal cytochrome P450 17alpha-hydroxylase-17, 20-lyase (CYP17) inhibitor (IC50: 4 nM).
    • $34
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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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  • K777
    T15641233277-99-1In house
    K777 is a potent, orally active, and irreversible inhibitor of cysteine protease, functioning as a potent CYP3A4 inhibitor (IC50 = 60 nM) and a selective CCR4 antagonist, which inhibits chemotaxis. K777 irreversibly inhibits Cruzain, the major cysteine protease of Trypanosoma cruzi, and cathepsins B and L, targeting cathepsin-mediated cell entry and exhibiting broad-spectrum antiviral activity. It inhibits EBOV and SARS-CoV pseudovirus entry with IC50 values of 0.87 nM and 0.68 nM, respectively.
    • $78
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  • Atazanavir sulfate
    T0100229975-97-7
    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.
    • $39
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  • AS1810722
    T9043909561-15-5
    AS1810722, a fused bicyclic pyrimidine derivative, is an orally active and potent inhibitor of STAT6, demonstrating an IC50 of 1.9 nM. It exhibits effective inhibition of CYP3A4, positioning it as a promising candidate for research into allergic diseases, including asthma and atopic conditions.
    • $106
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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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  • Oteseconazole
    T164121340593-59-0
    Oteseconazole (VT-1161) is an orally active anti-fungal agent. Oteseconazole displays no obvious effect on human CYP51. It also potently binds to and inhibits Candida albicans CYP51 (Kd, <39 nM).
    • $93
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  • Seviteronel
    T13312L1610537-15-9In house
    Seviteronel (VT-464) is a novel CYP17 cleavage enzyme inhibitor and androgen receptor antagonist used in breast and prostate cancer research.
    • $113 TargetMol
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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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  • Chrysosplenetin
    TJS1159603-56-5
    Chrysosplenetin is a metabolic inhibitor of artemisinin.
    • $55
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  • Lasiodin
    TN185428957-08-6
    Lasiodin (Lasiokaurin) is a diterpene compound from the plant Camellia sinensis that inhibits the proliferation of NPC cells. Lasiodin has antioxidant, antitumor and antibacterial activities, induces cell cycle length and apoptosis, induces cell migration and invasion, and can be used in the study of nasopharyngeal carcinoma.
    • $147
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  • Ranitidine
    T361066357-35-5
    Ranitidine (HSDB 3925) is a non-imidazole blocker of those histamine receptors that mediate gastric secretion (H2 receptors). It is used to treat gastrointestinal ulcers.
    • $35
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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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  • Ketoconazole
    T067965277-42-1
    Ketoconazole (R-41400), a CYP3A4 inhibitor, is an imidazole anti-fungal agent.
    • $33
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  • Azalanstat
    T25127143393-27-5In house
    Azalanstat (RS 21607) is an orally available selective mammalian lanosterol 14-alpha-demethylase inhibitor with hypocholesterolemic activity that inhibits cholesterol synthesis in HepG2 cells, human fibroblasts, hamster hepatocytes, and hamster livers through inhibition of the cytochrome P450 enzyme, lanosterol 14 alpha demethylase.
    • $1,520
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  • CYP1B1-IN-1
    T60723842122-33-2In house
    CYP1B1-IN-1 is a selective and highly potent cytochrome P450 1B1 (CYP1B1) inhibitor with potential anticancer and antitumor activity for breast cancer research.
    • $2,140
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  • TAK-700
    T6050426219-18-3
    TAK-700 (Orteronel) (Orteronel) is a potent and highly selective human 17, 20-lyase inhibitor with IC50 of 38 nM, exhibits >1000-fold selectivity over other CYPs (e.g. 11-hydroxylase and CYP3A4). Phase 3.
    • $34
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  • TP0472993
    T679162126874-77-7
    CYP4A11 CYP4F2-IN-2 is a potent and orally active dual inhibitor of cytochrome P450 (CYP) 4A11 and CYP4F2, with IC50 values of 140 nM and 40 nM, respectively. Extractable from liver and kidney, CYP4A11 CYP4F2-IN-2 has the potential to treat kidney diseases.
    • $44
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  • (Rac)-Brassinazole
    T7132224047-41-0
    (Rac)-Brassinazole are a class of phytohormones with essential roles in plant growth and development, including the promotion of stem elongation and cell division. Brassinazole is a triazole-type brassinosteroid biosynthesis inhibitor.
    • $54
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  • Itraconazole
    T101184625-61-6
    Itraconazole (R51211) is a triazole antifungal agent that inhibits cytochrome P-450-dependent enzymes necessary for ERGOSTEROL synthesis.
    • $34
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  • Tanshinone IIA sulfonate sodium
    T294669659-80-9
    Tanshinone IIA sulfonate sodium (Tanshinone IIA sodium sulfonate) is a water-soluble derivative of tanshinone IIA extracted from Savia miltiorrhiza; a potent negative allosteric modulator of the human purinergic receptor P2X7. Tanshinone IIA sulfonate sodium (12.5 μM) inhibits hypoxia-induced PKG and PPAR-γ downregulation in PASMCs and distal pulmonary arteries of rats.
    • $39
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  • N-Desmethyl-Apalutamide
    T121461332391-11-3
    N-Desmethyl-Apalutamide is a less potent antagonist of the androgen receptor, is an active Apalutamide metabolite.
    • $119
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  • Dronedarone
    T7056141626-36-0
    Dronedarone (SR 33589) is an amiodarone analogue which has an effective and promising treatment for Atrial fibrillation.
    • $30
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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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  • Bergamottin
    T5S06697380-40-7
    1. Bergamottin (5-Geranoxypsoralen) can significantly reduce blood glucose and increase glucose tolerance and insulin sensitivity in KK-Ay< sup>diabetic mice.
    • $40
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  • Humantenmine
    T2S066382354-38-9
    1. Humantenmine is a toxic compound isolated from Gelsemium elegans Benth . 2. Humantenmine and koumine may inhibit several CYP450 enzyme activities.
    • $40
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  • Ticagrelor
    T0179274693-27-5
    Ticagrelor (AR-C 126532XX), produced by AstraZeneca, is an inhibitor of platelet aggregation. Unlike clopidogrel, ticagrelor is not a prodrug required metabolic activation. The drug was approved for use in the European Union by the European Commission on December 3, 2010, and by the US FDA on July 20, 2011. Its trade names are Brilinta (US), Brilique(EU) and Possia(EU).
    • $40
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  • Demethyleneberberine
    T4S080025459-91-0
    Demethyleneberberine, which is composed of a potential antioxidant structure, could penetrate the membrane of mitochondria and accumulate in mitochondria either in vitro or in vivo.Demethyleneberberine suppresses CYP2E1, hypoxia inducible factor α, and inducible nitric oxide synthase, which contributes to oxidative stress and restored sirtuin 1 AMP-activated protein kinase peroxisome proliferator-activated receptor-γ coactivator-1α pathway-associated fatty acid oxidation in chronic ethanol-fed mice.
    • $61
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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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  • 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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  • 7-Ethoxyresorufin
    T215075725-91-7
    7-Ethoxyresorufin (Resorufin ethyl ether) (7-ER) is a fluorometric substrate and competitive inhibitor of cytochrome P450, particularly CYP1A1.
    • $30
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