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Isoforms Recommended: CYP3A4 CYP3
Results for "

CYP3A4

" in MedChemExpress (MCE) Product Catalog:

227

Inhibitors & Agonists

3

Fluorescent Dye

1

Biochemical Assay Reagents

34

Natural
Products

1

Recombinant Proteins

31

Isotope-Labeled Compounds

1

Antibodies

1

Oligonucleotides

Cat. No. Product Name Target Research Areas Chemical Structure
  • 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-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-RS03471

    Small Interfering RNA (siRNA) Others

    CYP3A4 Human Pre-designed siRNA Set A contains three designed siRNAs for CYP3A4 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.

    CYP3A4 Human Pre-designed siRNA Set A
    CYP3A4 Human Pre-designed siRNA Set A
  • 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-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-169217

    Cytochrome P450 Cancer
    CYP3A4-IN-4 (compound Δ,Λ-3), a Ru(II)−Ir(III) Conjugate, is a photoactive inhibitor of the major human drug metabolizing enzyme CYP3A4. CYP3A4-IN-4 containing the [Ru(tpy)(Me2bpy)] photocaging group showed an IC50 of 2.2 μM for inhibition of microsomal CYP3A4 under light conditions (λirr=530 nm, tirr=15 min). CYP3A4-IN-4 shows the phototherapeutic index (PI) for of 5.4 .
    CYP3A4-IN-4
  • 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-100243A

    (±)-Norcisapride; rel-Ticalopride

    Others Neurological Disease
    Norcisapride is a metabolite of cisapride (HY-14149). Norcisapride can be converted into UNK under CYP3A4 .
    Norcisapride
  • HY-119804

    Cytochrome P450 Neurological Disease
    Licopyranocoumarin is an isoflavonoid that shows CYP3A4 inhibitory activity with an IC50 of 32 μM. Licopyranocoumarin has potent neuroprotective activities .
    Licopyranocoumarin
  • HY-N10421

    (-)-Dihydrocubebin

    Others Others
    Dihydrocubebin is a compound isolated from Piper cubeba as potent and selective inhibitors against cytochrome P450 3A4 (CYP3A4) .
    Dihydrocubebin
  • HY-N0893S

    HZIV 81-2 d6

    Cytochrome P450 Autophagy Inflammation/Immunology Cancer
    Tetrahydrocurcumin-d6 is a deuterium labeled Tetrahydrocurcumin. Tetrahydrocurcumin is a Curcuminoid which displays inhibitory activity for CYP2C9 and CYP3A4[1].
    Tetrahydrocurcumin-d6
  • HY-163324

    Fluorescent Dye Others
    2-Me PeER (chloride) is a fluorogenic probe for CYP3A4 activity that can be used in living cells . Ex / Em = 520 / 550 nm
    2-Me PeER chloride
  • HY-156883

    Cytochrome P450 Others
    Dasatinib analog-1 (compound 5826) inhibits CYP3A4 viability with a Ki value of 5.4 μM. Dasatinib analog-1 blocks the formation of glutathione adducts .
    Dasatinib analog-1
  • HY-135331

    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-124364

    HBV Cytochrome P450 Infection Metabolic Disease
    RO6889678 is a highly potent HBV capsid formation inhibitor with a complex absorption, distribution, metabolism, and excretion (ADME) profile. RO6889678 is a potent inducer of CYP3A4 and coregulated proteins in human hepatocytes. RO6889678 is metabolized by a combination of CYP3A4-mediated oxidation and UDP-glucuronosyltransferase UGT1A3- and UGT1A1-mediated direct glucuronidation .
    RO6889678
  • 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-N9434

    Cytochrome P450 Metabolic Disease
    5,7,2',6'-Tetrahydroxyflavone is a natural flavonoid that inhibits hepatic testosterone 6β-hydroxylation (CYP3A4) activity with an IC50 of 7.8 μM .
    5,7,2',6'-Tetrahydroxyflavone
  • 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-125505

    Factor Xa Cardiovascular Disease
    BI-11634 is a factor Xa inhibitor. BI-11634 is metabolized by CYP3A4 to form one major metabolite and this reaction is inhibited by Quinidine (HY-B1751H) with a Ki of 7 µM .
    BI-11634
  • 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-100638A

    NPC hydrochloride

    Drug Metabolite Cancer
    RPR132595A (NPC) hydrochloride is an active metabolite of CPT-11, which is generated by cytochrome P-450 3A4 (CYP3A4) and finally excreted through urine .
    RPR132595A hydrochloride
  • HY-100665
    Dehydroaripiprazole
    1 Publications Verification

    OPC-14857; DM-14857

    5-HT Receptor Neurological Disease
    Dehydroaripiprazole (OPC-14857) is an active metabolite of Aripiprazole. Aripiprazole is an antipsychotic agent and is metabolized by CYP3A4 and CYP2D6 forming mainly Dehydroaripiprazole. Dehydroaripiprazole has with antipsychotic activity equivalent to Aripiprazole .
    Dehydroaripiprazole
  • HY-19958

    Sodium Channel Neurological Disease
    XEN907 is a potent and spirooxindole blocker of NaV1.7, with an IC50 of 3 nM. XEN907 also inhibits CYP3A4 in a recombinant human enzyme assay. XEN907 can be used for the research of pain .
    XEN907
  • HY-113575

    OPC-14857 hydrochloride; DM-14857 hydrochloride

    5-HT Receptor Neurological Disease
    Dehydroaripiprazole (OPC-14857) hydrochloride is an active metabolite of Aripiprazole. Aripiprazole is an antipsychotic agent and is metabolized by CYP3A4 and CYP2D6 forming mainly Dehydroaripiprazole hydrochloride. Dehydroaripiprazole hydrochloride has with antipsychotic activity equivalent to Aripiprazole .
    Dehydroaripiprazole hydrochloride
  • 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-14874
    Topiroxostat
    5 Publications Verification

    FYX-051

    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-B0352B

    (R)-Org3770; (R)-6-Azamianserin

    5-HT Receptor Neurological Disease
    (R)-Mirtazapine ((R)-Org3770) is a R(−)-enantiomer of Mirtazapine with antinociceptive properties in an animal model of acute thermal nociception. (R)-Mirtazapine is a 5-HT3 receptor antagonist. (R)-Mirtazapine is mainly metabolized by CYP3A4 .
    (R)-Mirtazapine
  • HY-147810

    5-HT Receptor Neurological Disease
    5-HT7 receptor ligand 1 (Compound 5c) is a 5-HT7 receptor ligand with a Ki of 8 nM. 5-HT7 receptor ligand 1 is not hepatotoxic and exhibit moderate potential interaction with other agents metabolized by CYP3A4 or CYP2D6 .
    5-HT7 receptor ligand 1
  • HY-119996

    Others Inflammation/Immunology
    AR-C141990 (Compound 30) is a potent blocker of the monocarboxylate transporter MCT1 with a Ki of 4.8 nM. AR-C141990 (Compound 30) inhibits CYP3A4 and CYP2C9 with IC50 values of 16 μM .
    AR-C141990
  • HY-B0105A

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

    Fungal Cytochrome P450 Infection
    (+)-Ketoconazole ((+)-R 41400) is an imidazole anti-fungal agent, a CYP3A4 inhibitor.
    (+)-Ketoconazole
  • HY-168210

    Fungal Infection
    Antifungal agent 122 (compound 201) is a potent and broad-spectrum antifungal agent. Antifungal agent 122 prevents fungal phase transition and the formation of fungal biofilm. Antifungal agent 122 inhibits CYP3A4-M and CYP3A4-M enzyme activity with IC50 values of 2.11, 4.53 µM. Antifungal agent 122 shows no cytotoxicity .
    Antifungal agent 122
  • HY-17508
    Clarithromycin
    10+ 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-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-B2015S

    Cytochrome P450 Parasite Infection
    Carbosulfan-d18 is the deuterium labeled Carbosulfan. Carbosulfan inhibited relatively potently CYP3A4 and moderately CYP1A1/2 and CYP2C19 in pooled HLM (human livers). Carbosulfan activation is predominantly catalyzed in humans by CYP3A4.
    Carbosulfan-d18
  • HY-100620

    APC

    Topoisomerase Cholinesterase (ChE) Cancer
    RPR121056 (APC) is a metabolite of Irinotecan (CPT-11), which is generated by CYP3A4. Irinotecan (CPT-11) is an antineoplastic agent that inhibits topoisomerase type I, causing cell death, and is widely used in the treatment of colorectal cancer. Irinotecan also directly inhibits AChE .
    RPR121056
  • HY-W420344

    Others Others
    Dehydroindapamide is the indole form of Indapamide (HY-B0259). Dehydroindapamide standard can be used to quantitatively measure the Indapamide turnover rate by CYP3A4, which was approximately 10-fold higher than that of Indoline (HY-Y0788), and slightly enhanced affinity for CYP3A4 .
    Dehydroindapamide
  • HY-14874R

    Xanthine Oxidase Cytochrome P450 Metabolic Disease
    Topiroxostat (Standard) is the analytical standard of Topiroxostat. This product is intended for research and analytical applications. 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 (Standard)
  • HY-N0779

    Isosilybinin

    Cytochrome P450 Cancer
    Isosilybin (Isosilybinin) is a flavonoid from Silybum marianum; inhibits CYP3A4 induction with an IC50 of 74 μM.
    Isosilybin
  • HY-A0064
    Verapamil hydrochloride
    Maximum Cited Publications
    54 Publications Verification

    (±)-Verapamil hydrochloride; CP-16533-1 hydrochloride

    Calcium Channel P-glycoprotein Cytochrome P450 Cardiovascular Disease Cancer
    Verapamil hydrochloride ((±)-Verapamil hydrochloride) is a calcium channel blocker and a potent and orally active first-generation P-glycoprotein (P-gp) inhibitor. Verapamil hydrochloride also inhibits CYP3A4. Verapamil hydrochloride has the potential for high blood pressure, heart arrhythmias and angina research .
    Verapamil hydrochloride
  • HY-14275
    Verapamil
    Maximum Cited Publications
    54 Publications Verification

    (±)-Verapamil; CP-16533-1

    Calcium Channel P-glycoprotein Cytochrome P450 Metabolic Disease Cancer
    Verapamil ((±)-Verapamil) is a calcium channel blocker and a potent and orally active first-generation P-glycoprotein (P-gp) inhibitor. Verapamil also inhibits CYP3A4. Verapamil has the potential for high blood pressure, heart arrhythmias and angina research .
    Verapamil
  • HY-B0352BS

    (R)-Org3770 d3; (R)-6-Azamianserin d3

    Isotope-Labeled Compounds 5-HT Receptor Neurological Disease
    (R)-Mirtazapine-d3 is a deuterium labeled (R)-Mirtazapine. (R)-Mirtazapine is a R(−)-enantiomer of Mirtazapine with antinociceptive properties in an animal model of acute thermal nociception. (R)-Mirtazapine is a 5-HT3 receptor antagonist. (R)-Mirtazapine is mainly metabolized by CYP3A4[1].
    (R)-Mirtazapine-d3
  • HY-153989

    Ras Cytochrome P450 Cancer
    SOS1-IN-16 (Comp 54) is a selective inhibitor of SOS1 with an IC50 of 7.2 nM. SOS1-IN-16 has inhibitory activity of CYP3A4 when using testosterone as a substrate, with an IC50 of 8.9μM. SOS1-IN-16 can be used for cancer research .
    SOS1-IN-16
  • HY-B0105
    Ketoconazole
    15+ 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-163324A

    Cytochrome P450 Others
    2-Me PeER is a rhodamine dye-based fluorescent probe that detects CYP3A4 activity. In fluorescence-activated cell sorting (FACS) based on CYP3A4 activity, homogeneous and functional human induced pluripotent stem cell (hiPSC)-derived hepatocytes and intestinal epithelial cells can be obtained with the aid of 2-Me PeER .
    2-Me PeER
  • HY-111202

    TSH-888

    Cytochrome P450 Inflammation/Immunology
    Pyributicarb, a carbamate-type herbicide, is a potent activator of both CYP3A4 gene and human pregnane X receptor (hPXR).
    Pyributicarb
  • HY-146458

    Bacterial Cytochrome P450 Infection
    Antibacterial agent 102 (compound 32) possesses potent in vitro and in vivo antibacterial activity, with MICs < 0.5 μg/mL in Staphylococcus aureus (S. aureus). Antibacterial agent 102 also moderately inhibits CYP3A4 with an IC50 value of 6.148 μM. Antibacterial agent 102 can reduce Methicillin-resistant Staphylococcus aureus (MRSA) load in thigh infected mice .
    Antibacterial agent 102
  • HY-W420344R

    Others Others
    Dehydroindapamide (Standard) is the analytical standard of Dehydroindapamide. This product is intended for research and analytical applications. Dehydroindapamide is the indole form of Indapamide (HY-B0259). Dehydroindapamide standard can be used to quantitatively measure the Indapamide turnover rate by CYP3A4, which was approximately 10-fold higher than that of Indoline (HY-Y0788), and slightly enhanced affinity for CYP3A4 .
    Dehydroindapamide (Standard)
  • HY-N8382

    Cytochrome P450 Neurological Disease
    Chalepensin, a furanocoumarin, is a competitive CYP2A6 inhibitor. Chalepensin also inhibits human CYP1A1, CYP1A2, CYP2A13, CYP2C9, CYP2D6, CYP2E1, and CYP3A4 to different extents .
    Chalepensin
  • 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-120696

    ML368

    Cytochrome P450 Parasite Infection
    SR9186 (ML368) is a potent CYP3A4 inhibitor with IC50 s for inhibition of midazolam → 1′hydroxymidazolam, testosterone → 6β-hydroxytestosterone, and vincristine → vincristine M1 of 9, 4, and 38 nM, respectively. SR-9186 inhibits liver-stage development of P. falciparum to block ivermectin metabolism .
    SR9186

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