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Isoforms Recommended: CYP3A4 CYP3
Results for "

CYP 3A4

" in MedChemExpress (MCE) Product Catalog:

328

Inhibitors & Agonists

1

Screening Libraries

3

Fluorescent Dye

1

Biochemical Assay Reagents

51

Natural
Products

1

Recombinant Proteins

51

Isotope-Labeled Compounds

3

Antibodies

1

Oligonucleotides

1

GMP Molecules

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-B0105
    Ketoconazole
    25+ Cited Publications

    Ketoconazol; R 41400

    Fungal Cytochrome P450 Ras Bacterial Infection Cancer
    Ketoconazole (R-41400) is an imidazole anti-fungal agent, a CYP3A4 and CYP24A1 inhibitor.
    Ketoconazole
  • HY-17356
    Fenofibrate
    30+ Cited Publications

    PPAR Cytochrome P450 Autophagy Cardiovascular Disease Cancer
    Fenofibrate is a selective PPARα agonist with an EC50 of 30 μM. Fenofibrate also inhibits human cytochrome P450 isoforms, with IC50s of 0.2, 0.7, 9.7, 4.8 and 142.1 μM for CYP2C19, CYP2B6, CYP2C9, CYP2C8, and CYP3A4, respectively.
    Fenofibrate
  • HY-17508
    Clarithromycin
    20+ Cited Publications

    Bacterial Cytochrome P450 Autophagy Antibiotic Infection Cancer
    Clarithromycin has a broad spectrum of antimicrobial activity. Clarithromycin inhibits the CYP3A4-catalyzed triazolam alpha-hydroxylation with the IC50 (Ki) value of 56 (43) μM . Clarithromycin significantly inhibits the HERG potassium current .Clarithromycin affects the autophagic flux by impairing the signaling pathway linking hERG1 and PI3K .
    Clarithromycin
  • HY-124527
    HET0016
    5+ Cited Publications

    Cytochrome P450 Cardiovascular Disease Cancer
    HET0016 is a potent and selective 20-hydroxyeicosatetraenoic acid (20-HETE) synthase inhibitor, with IC50 values of 17.7 nM, 12.1 nM and 20.6 nM for recombinant CYP4A1-, CYP4A2- and CYP4A3-catalyzed 20-HETE synthesis, respectively. HET0016 also is a selective CYP450 inhibitor, which has been shown to inhibit angiogenesis and tumor growth .
    HET0016
  • HY-N0893
    Tetrahydrocurcumin
    2 Publications Verification

    HZIV 81-2

    Cytochrome P450 Autophagy Endogenous Metabolite Inflammation/Immunology Cancer
    Tetrahydrocurcumin is a Curcuminoid found in turmeric (Curcuma longa) that is produced by the reduction of Curcumin. Tetrahydrocurcumin inhibit CYP2C9 and CYP3A4.
    Tetrahydrocurcumin
  • HY-13600
    Clobetasol propionate
    1 Publications Verification

    Cytochrome P450 Inflammation/Immunology Endocrinology Cancer
    Clobetasol propionate is a potent and selective CYP3A5 inhibitor with an IC50 of 0.206 μM. Clobetasol propionate has no inhibiting on CYP3A4 or other major CYPs. Clobetasol propionate is a corticosteroid and has the potential for psoriasis and other dermatoses research .
    Clobetasol propionate
  • HY-B0105A

    (+)-Ketoconazol; (+)-R 41400

    Fungal Cytochrome P450 Infection
    (+)-Ketoconazole ((+)-R 41400) is an imidazole anti-fungal agent, a CYP3A4 inhibitor.
    (+)-Ketoconazole
  • HY-18642

    PF-4981517

    Cytochrome P450 Others
    CYP3cide (PF-4981517) is a potent, selective and time-dependent inhibitor of cytochrome P4503A4 (CYP3A4). The IC50 values for Midazolam 1’-hydroxylase activity are 0.03 μM, 17 μM, and 71 μM for CYP3A4, CYP3A5, and CYP3A7, respectively. CYP3cide can be used to distinguish the contributions of CYP3A4 versus CYP3A5 on agent metabolism .
    CYP3cide
  • HY-N0598
    Ginsenoside F1
    1 Publications Verification

    20(S)-Ginsenoside F1

    Cytochrome P450 Endogenous Metabolite Cancer
    Ginsenoside F1, an enzymatically modified derivative of Ginsenoside Rg1, demonstrates competitive inhibition of CYP3A4 activity and weaker inhibition of CYP2D6 activity.
    Ginsenoside F1
  • HY-14874
    Topiroxostat
    5+ Cited Publications

    FYX-051

    MOFs Xanthine Oxidase Cytochrome P450 Metabolic Disease
    Topiroxostat (FYX-051) is a potent and orally active xanthine oxidoreductase (XOR) inhibitor with an IC50 value of 5.3 nM and a Ki value of 5.7 nM. Topiroxostat exhibits weak CYP3A4-inhibitory activity (18.6%). Topiroxostat has the potential for hyperuricemia treatment .
    Topiroxostat
  • HY-N5132

    Cytochrome P450 Others
    (-)-Fenchone is a bicyclic monoterpene and serves as a substrate for human liver microsomal cytochrome P450 enzymes CYP2A6 and CYP2B6. (-)-Fenchone is not metabolized by human CYP1A1, CYP1A2, CYP1B1, CYP2C8, CYP2C9, CYP2C19, CYP2D6, CYP2E1, or CYP3A4 enzymes. (-)-Fenchone undergoes hydroxylation to produce 6-exo-hydroxyfenchone, 6-endo-hydroxyfenchone, and 10-hydroxyfenchone. During the metabolism of (-)-Fenchone, CYP2A6 may play a more important role than CYP2B6 .
    (-)-Fenchone
  • HY-N0779
    Isosilybin
    2 Publications Verification

    Isosilybinin

    Cytochrome P450 Cancer
    Isosilybin (Isosilybinin) is a flavonoid from Silybum marianum; inhibits CYP3A4 induction with an IC50 of 74 μM.
    Isosilybin
  • HY-N6023

    Cytochrome P450 Pregnane X Receptor (PXR) Others
    Thermopsoside is a CYP450 isoenzyme inhibitor and PXR activator. Thermopsoside inhibits CYP3A4, CYP2C19, CYP2D6 and CYP2C9 with IC50 values of 6.0 μM, 9.5 μM, 12.0 μM and 32.0 μM, respectively .
    Thermopsoside
  • HY-113482

    1β-OH-DCA

    Endogenous Metabolite Cytochrome P450 Metabolic Disease
    1β-Hydroxydeoxycholic acid (1β-OH-DCA), a secondary bile acid, is a CYP3A biomarker. Deoxycholic acid is specifically metabolized into 1β-Hydroxydeoxycholic acid by CYP3A4 and CYP3A7 using recombinant human CYP450 enzymes .
    1β-Hydroxydeoxycholic acid
  • HY-W013268

    (+)-N-3-Benzylnirvanol

    Cytochrome P450 Metabolic Disease
    (S)-(+)-N-3-Benzylnirvanol ((+)-N-3-Benzylnirvanol) is a selective and competitive cytochrome P450 (CYP) isoform CYP2C19 inhibitor with a Ki of 250 nM. (S)-(+)-N-3-Benzylnirvanol has low activity against CYP1A2, CYP2A6, CYP2C8, CYP2C9, CYP2D6, CYP2E1, and CYP3A4 .
    (S)-(+)-N-3-Benzylnirvanol
  • HY-135331
    N-Desmethyl-Apalutamide
    1 Publications Verification

    Androgen Receptor Cytochrome P450 Cancer
    N-Desmethyl Apalutamide is an active metabolite of Apalutamide. N-Desmethyl Apalutamide is a less potent antagonist of the androgen receptor and is responsible for one-third of the activity of Apalutamide. The formation of N-Desmethyl Apalutamide mediated predominantly by CYP2C8 and CYP3A4. N-Desmethyl Apalutamide is moderate to strong CYP3A4 and CYP2B6 inducer and has an excellent plasma-proteins bound concentration .
    N-Desmethyl-Apalutamide
  • HY-116862

    DBF

    Cytochrome P450 Fluorescent Dye Others
    Dibenzylfluorescein (DBF) is a fluorogenic probe (Fluoresecent dye) that acts as a substrate for specific cytochrome P450 (CYP) isoforms, including CYP3A4, CYP2C8, CYP2C9, CYP2C19, and aromatase (CYP19). Dibenzylfluorescein is typically used near its Km value of 0.87-1.9 μM (Ex=485 nm,Em=535 nm). Dibenzylfluorescein is used to detect changes in CYP catalytic activity caused by drugs or disease .
    Dibenzylfluorescein
  • HY-B0105R

    Ketoconazol (Standard); R 41400 (Standard)

    Reference Standards Fungal Cytochrome P450 Ras Bacterial Infection Cancer
    Ketoconazole (Standard) is the analytical standard of Ketoconazole. This product is intended for research and analytical applications. Ketoconazole (R-41400) is an imidazole anti-fungal agent, a CYP3A4 and CYP24A1 inhibitor.
    Ketoconazole (Standard)
  • HY-N8354

    6′,7′-DHB

    Cytochrome P450 Cardiovascular Disease
    6',7'-Dihydroxybergamottin (6′,7′-DHB), a furanocoumarin, is a potent CYP3A4 inhibitor .
    6',7'-Dihydroxybergamottin
  • HY-N2262

    Cytochrome P450 Cancer
    8-Geranyloxypsoralen is a furanocoumarin isolated from grapefruit, acts as a potent inhibitor of P450 3A4 (CYP3A4) with an IC50 of 3.93 μM .
    8-Geranyloxypsoralen
  • HY-150574

    Cytochrome P450 Infection
    CYP3A4-IN-1 (compound 5a) is a potent cytochrome P450 3A4 (CYP3A4) inhibitor with an IC50 value of 0.085 µM .
    CYP3A4-IN-1
  • HY-124542

    Drug Metabolite Apoptosis Cancer
    5-Hydroxydiclofenac is a major metabolite of Diclofenac (HY-15036). 5-Hydroxydiclofenac is formed by the cytochrome P450 (CYP) isoforms CYP3A4, CYP2C189, CYP2C19, and CYP2C8. 5-Hydroxydiclofenac shows apoptotic effects in hepatocytes .
    5-Hydroxydiclofenac
  • HY-10505
    Orteronel
    2 Publications Verification

    TAK-700

    Cytochrome P450 Cancer
    Orteronel (TAK-700) is a highly selective inhibitor of human 17,20-lyase (CYP17) with IC50 of 38 nM, and exhibits >1000-fold selectivity over other CYPs such as 11-hydroxylase and CYP3A4 .
    Orteronel
  • HY-17356S

    Isotope-Labeled Compounds PPAR Cytochrome P450 Autophagy Cardiovascular Disease Cancer
    Fenofibrate-d6 is the deuterium labeled Fenofibrate. Fenofibrate is a selective PPARα agonist with an EC50 of 30 μM. Fenofibrate also inhibits human cytochrome P450 isoforms, with IC50s of 0.2, 0.7, 9.7, 4.8 and 142.1 μM for CYP2C19, CYP2B6, CYP2C9, CYP2C8, and CYP3A4, respectively.
    Fenofibrate-d6
  • HY-114411

    Estrogen Receptor/ERR Cancer
    ERRγ inverse agonist 1 (Compound 12) is a selective ERRγ inverse agonist with an IC50 value of 0.040 μM against ERRγ. ERRγ inverse agonist 1 inhibits the activity of ERRγ at the functional level. ERRγ inverse agonist 1 can be used in the research of anaplastic thyroid cancer .
    ERRγ inverse agonist 1
  • HY-120425

    Environmental Pollutants Insecticide Infection
    Ethiprole is an insecticide.Metabolic sulfones are produced faster than Fipronil (HY-B0822) in CYP3A4-expressing cells and in vivo in mouse brain and liver.Ethiprole's sulfide, sulfoxide, sulfone and desulfinyl derivatives have better biological activity .
    Ethiprole
  • HY-135810

    Desethylhydroxychloroquine

    CHIKV Influenza Virus Parasite Infection Inflammation/Immunology
    Cletoquine (Desethylhydroxychloroquine) is a major active metabolite of Hydroxychloroquine. Cletoquine is produced in the liver by CYP2D6, CYP3A4, CYP3A5, and CYP2C8 isoenzymes. Cletoquine is also a Chloroquine derivative and has the ability to against the chikungunya virus (CHIKV). Cletoquine has antimalarial effects and has the potential for autoimmune diseases treatment .
    Cletoquine
  • HY-113031

    16α-Hydroxy-DHEA; 16α-OH-DHEA; 16α-hydroxy DHEA

    Cytochrome P450 Endocrinology
    16a-Hydroxydehydroisoandrosterone (16α-Hydroxy-DHEA) is a metabolite of the endogenous steroid hormone dehydroepiandrosterone. 16α-hydroxy Dehydroepiandrosterone is formed from dehydroepiandrosterone via 16-hydroxylation by the cytochrome P450 (CYP) isoforms CYP3A4 and CYP3A5 in adult human liver microsomes, as well as by fetal recombinant CYP3A7. It is a precursor to fetal estrogens, including estriol.
    16a-Hydroxydehydroisoandrosterone
  • HY-17356R
    Fenofibrate (Standard)
    30+ Cited Publications

    Reference Standards PPAR Cytochrome P450 Autophagy Cardiovascular Disease Cancer
    Fenofibrate (Standard) is the analytical standard of Fenofibrate. This product is intended for research and analytical applications. Fenofibrate is a selective PPARα agonist with an EC50 of 30 μM. Fenofibrate also inhibits human cytochrome P450 isoforms, with IC50s of 0.2, 0.7, 9.7, 4.8 and 142.1 μM for CYP2C19, CYP2B6, CYP2C9, CYP2C8, and CYP3A4, respectively.
    Fenofibrate (Standard)
  • HY-N16471

    5-HT Receptor Cytochrome P450 Neurological Disease
    Escholtzine is an Alkaloid. Escholtzine can be isolated from Eschscholzia californica. Escholtzine is a CYP3A4 inhibitor, 5-HT1A receptor inhibitor with a CYP3A4 IC50 of 13.4 μM, 5-HT1A EC50 of 11 μM. Escholtzine can be used for the research of anxiety, depression .
    Escholtzine
  • HY-133152

    DM-3411

    5-HT Receptor Dopamine Receptor Neurological Disease
    Brexpiprazole S-oxide (DM-3411) is a main metabolite of Brexpiprazole and is metabolized by cytochrome P450 3A4 (CYP3A4). Brexpiprazole is an atypical antipsychotic agent and a partial agonist of human 5-HT1A and dopamine receptor with Kis of 0.12 nM and 0.3 nM, respectively. Brexpiprazole is also a 5-HT2A receptor antagonist with a Ki of 0.47 nM .
    Brexpiprazole S-oxide
  • HY-107461

    Glucocorticoid Receptor Cardiovascular Disease
    LY2623091 is a mineralocorticoid receptor antagonist for the treatment of refractory hypertension. LY2623091 exhibits CYP3A4-dependent clearance and synergistic effects with CYP3A4 inhibitors .
    LY2623091
  • HY-116780A

    Cytochrome P450 Neurological Disease
    Prothipendyl hydrochloride is a tricyclic azaphenothiazine neuroleptic agent. Prothipendyl hydrochloride is a substrate of the CYP isozymes CYP1A2, CYP2D6, CYP2C19 and CYP3A4. Prothipendyl hydrochloride has sedating and psychomotorically damping effects. Prothipendyl hydrochloride can be used for psychomotoric agitation, sleep disorder and anxiety research .
    Prothipendyl hydrochloride
  • HY-N8382

    Cytochrome P450 Parasite Insecticide Infection
    Chalepensin is a nematicide and CYP inhibitor. Chalepensin inhibits CYP2A6, CYP1A1, CYP1A2, CYP2A13, CYP2C9, CYP2D6, CYP2E1, and CYP3A4 to varying degrees, with IC50 values of 82.3 μM, 2.86 μM, 3.01 μM, 0.21 μM, 6.58 μM, 1.67 μM, 61.1 μM, and 61.7 μM, respectively. Chalepensin potently and selectively kills third-stage infective larvae of Strongyloides venezuelensis .
    Chalepensin
  • HY-16785B

    INXN-1001 (S enantiomer); RG-115932 (S enantiomer)

    Interleukin Related Cancer
    Veledimex S enantiomer (INXN-1001 S enantiomer) is the S enantiomer of veledimex. Veledimex is an oral activator ligand for a proprietary gene therapy promoter system, and a moderate inhibitor of and substrate for CYP3A4/5 .
    Veledimex (S enantiomer)
  • HY-N0893R

    HZIV 81-2 (Standard)

    Reference Standards Cytochrome P450 Autophagy Endogenous Metabolite Inflammation/Immunology Cancer
    Tetrahydrocurcumin (Standard) is the analytical standard of Tetrahydrocurcumin. This product is intended for research and analytical applications. Tetrahydrocurcumin is a Curcuminoid found in turmeric (Curcuma longa) that is produced by the reduction of Curcumin. Tetrahydrocurcumin inhibit CYP2C9 and CYP3A4.
    Tetrahydrocurcumin (Standard)
  • HY-W587878

    Cytochrome P450 Pyruvate Kinase Fungal Apoptosis Insecticide Infection Cancer
    Thujopsene is the inhibitor for cytochrome P450, that inhibits CYP2B6, CYP3A4, CYP2C19, CYP2C8, CYP2C9 with IC50s of 1.3, 12.6, 13.6, 29.8, and 44.9 μM, respectively. Thujopsene binds to PKM2, inhibits the metabolism pathway of cancer cell, induces apoptosis in MKN45, thereby exhibiting antitumor efficacy. Thujopsene exhibits anti-termite and antifungal activities through autoxidation .
    Thujopsene
  • HY-150580

    Cytochrome P450 Inflammation/Immunology Cancer
    CYP3A4-IN-2 is a specific inhibitor of cytochrome P450 3A4 (CYP3A4) with the IC50 value of 0.055 μM. CYP3A4-IN-2 is a ritonavir analogue with increased hydrophobicity of the R2 side group and stronger inhibitory effect compared to ritonavir. CYP3A4-IN-2 can be used as an antiviral agent and immunosuppressants .
    CYP3A4-IN-2
  • HY-133152S

    DM-3411 d8

    Isotope-Labeled Compounds 5-HT Receptor Dopamine Receptor Neurological Disease
    Brexpiprazole S-oxide-d8 (DM-3411 D8) is a deuterium labeled Brexpiprazole S-oxide (HY-133152). Brexpiprazole S-oxide is a main metabolite of Brexpiprazole and is metabolized by cytochrome P450 3A4 (CYP3A4). Brexpiprazole is an atypical antipsychotic agent and a partial agonist of human 5-HT1A and dopamine receptor with Kis of 0.12 nM and 0.3 nM, respectively. Brexpiprazole is also a 5-HT2A receptor antagonist with a Ki of 0.47 nM .
    Brexpiprazole S-oxide-d8
  • HY-135161

    Drug Metabolite Others
    EDDP perchlorate is an N-desmethyl metabolite of Methadone by intestinal, hepatic, and cytochrome P450 (CYP) 3A4 .
    EDDP perchlorate
  • HY-100638

    NPC

    Drug Metabolite Cancer
    RPR132595A (NPC) is an active metabolite of CPT-11, which is generated by cytochrome P-450 3A4 (CYP3A4) and finally excreted through urine .
    RPR132595A
  • HY-N3090

    Cytochrome P450 Metabolic Disease
    Peucedanol is a non-competitive inhibitor of CYP3A4 with a Ki value of 4.07 μM and a competitive inhibitor of CYP1A2 and CYP2D6 with Ki values of 3.39 μM and 6.77 μM, respectively .
    Peucedanol
  • HY-B0105S1

    Ketoconazol-d4; R 41400-d4

    Fungal Cytochrome P450 Ras Infection Cancer
    Ketoconazole-d4 is the deuterium labeled Ketoconazole. Ketoconazole (R-41400) is an imidazole anti-fungal agent, a CYP3A4 and CYP24A1 inhibitor.
    Ketoconazole-d4
  • HY-W754151

    Isotope-Labeled Compounds Others
    N-Desmethyl apalutamide-d4 is the deuterium-labeled N-Desmethyl-Apalutamide (HY-135331). N-Desmethyl Apalutamide is an active metabolite of Apalutamide. N-Desmethyl Apalutamide is a less potent antagonist of the androgen receptor and is responsible for one-third of the activity of Apalutamide. The formation of N-Desmethyl Apalutamide mediated predominantly by CYP2C8 and CYP3A4. N-Desmethyl Apalutamide is moderate to strong CYP3A4 and CYP2B6 inducer and has an excellent plasma-proteins bound concentration .
    N-Desmethyl apalutamide-d4
  • HY-122508

    Drug Metabolite Neurological Disease
    Hydroxyebastine is an Ebastine (HY-B0674) (a histamine H1-receptor antagonist) metabolite. Hydroxyebastine is metabolized to Carebastine (HY-121356) by CYP2J2 and CYP3A4 .
    Hydroxyebastine
  • HY-150581

    Cytochrome P450 Infection Inflammation/Immunology
    CYP3A4-IN-3 is a high-affinity specific inhibitor of cytochrome P450 3A4 (CYP3A4) with the IC50 value of 0.075 μM. CYP3A4-IN-3 is a ritonavir analogue, but with a simpler structure and twice the inhibitory effect of ritonavir. CYP3A4-IN-3 is used as an antiviral agent and immunosuppressant .
    CYP3A4-IN-3
  • HY-W075315

    MOFs Xanthine Oxidase Cytochrome P450 Metabolic Disease
    Xanthine oxidoreductase-IN-6 (Compound 4) is an orally active xanthine oxidoreductase (XOR) inhibitor with an IC50 of 170 nM. Xanthine oxidoreductase-IN-6 can block the final step of uric acid biosynthesis and lower serum uric acid levels. Xanthine oxidoreductase-IN-6 also shows Cytochrome P450 3A4 (CYP3A4) inhibitory activity. Xanthine oxidoreductase-IN-6 can be used for the research of hyperuricemia .
    Xanthine oxidoreductase-IN-6
  • HY-175345

    Parasite Infection
    CYP3A4-IN-5 (Compound 5p) is a potent Leishmania major pteridine reductase 1 (Lm PTR1) inhibitor (IC50=12.77 µM). CYP3A4-IN-5 is promising for research of parasite infection .
    CYP3A4-IN-5
  • HY-146177

    Bacterial Cytochrome P450 Infection
    CYP3A4 enzyme-IN-1 (compound 59) is a potent antibacterial agent, with a MIC of 1 μg/mL for MRSA. CYP3A4 enzyme-IN-1 exhibits low to moderate inhibitory effects on CYP1A2, CYP2E1, CYP2D6, and CYP3A4 enzymes .
    CYP3A4 enzyme-IN-1
  • HY-N10421

    (-)-Dihydrocubebin

    Cytochrome P450 Others
    Dihydrocubebin is a compound isolated from Piper cubeba as potent and selective inhibitors against cytochrome P450 3A4 (CYP3A4) .
    Dihydrocubebin

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