2. Search Result
Search Result
Results for "

human CYP2D6

" in MedChemExpress (MCE) Product Catalog:

30

Inhibitors & Agonists

1

Peptides

5

Natural
Products

2

Isotope-Labeled Compounds

1

Oligonucleotides

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-157421
    Nampt activator-4

    		NAMPT Metabolic Disease
    Nampt activator-4 is an orally active NAMPT activator, with an EC50 of 58 nM and a Ka of 85.38 nM against human NAMPT. Nampt activator-4 effectively relieves the feedback inhibition of nicotinamide and NAD +, thereby enhancing enzymatic activity and significantly increasing intracellular NAD + levels. Nampt activator-4 exhibits moderate stability in human and mouse liver microsomes. Nampt activator-4 shows low to moderate inhibitory effects on cytochrome P450 (especially CYP3A4). Nampt activator-4 can be used for the research of type 2 diabetes and related metabolic disorders .
    Nampt activator-4
  • HY-N2129
    N-Nornuciferine
    1 Publications Verification

    		 Cytochrome P450 Cholinesterase (ChE) Cardiovascular Disease Metabolic Disease
    N-Nornuciferine is an orally active, blood-brain barrier-permeable CYP2D6 inhibitor, with an IC50 of 3.76 μM and a Ki of 2.34 μM against human CYP2D6. N-Nornuciferine also acts as a BChE inhibitor, showing an IC50 of 5.6 μM in mice . N-Nornuciferine can be used in the research of neurological-related diseases .
    N-Nornuciferine
  • HY-N5132
    (-)-Fenchone

    		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-15163
    Zotiraciclib
    2 Publications Verification

    TG02; SB1317

    		 JAK CDK FLT3 Cancer
    Zotiraciclib (TG02; SB1317) is an orally active JAK2/FLT3/CDK2 inhibitor with IC50 values of 13 nM, 73 nM and 56 nM , respectively. Zotiraciclib inhibits cancer cell proliferation, tumor growth and the activity of CYP2D6. Zotiraciclib exhibits high plasma protein binding rate, Caco-2 permeability and tissue distribution capacity, as well as metabolic stability in human and canine liver microsomes. Zotiraciclib achieves tumor growth inhibition in nude mouse models of colon cancer and lymphoma xenografts. Zotiraciclib can be used for research related to colon cancer, B-cell lymphoma, advanced leukemia, acute leukemia and multiple myeloma .
    Zotiraciclib
  • HY-W040468
    2-Phenyl-2-(1-piperidinyl)propane

    		Cytochrome P450 Metabolic Disease
    2-Phenyl-2-(1-piperidinyl)propane is a selective and reversible human CYP2B6 inhibitor with an IC50 of 5.1 μM and a Ki of 5.6. 2-Phenyl-2-(1-piperidinyl)propane inhibits CYP2D6 (IC50=74 μM), CYP3A (IC50=200 μM) .
    2-Phenyl-2-(1-piperidinyl)propane
  • HY-128914
    Tubulysin

    		ADC Payload Microtubule/Tubulin Apoptosis Cancer
    Tubulysin is a microtubule destabilizer that binds to the β-tubulin peptide site adjacent to the vinca alkaloid binding site and inhibits tubulin polymerization. Tubulysin induces apoptosis and exhibits antiproliferative activity against a variety of human cancer cells, including multidrug-resistant strains. Tubulysin can be conjugated to antibodies via a disulfide-containing quaternary ammonium linker for ADC synthesis . Tubulysin is applicable to tumor-related research .
    Tubulysin
  • HY-100064
    O-Desmethyl gefitinib

    		EGFR Cancer
    O-Desmethyl gefitinib is an active metabolite of Gefitinib in human plasma. The formation of O-desmethyl gefitinib is dependent on CYP2D6 activity. O-desmethyl gefitinib inhibits EGFR with an IC50 of 36 nM in subcellular assays .
    O-Desmethyl gefitinib
  • HY-16718
    Dagrocorat

    PF-00251802

    		 Glucocorticoid Receptor Cytochrome P450 Inflammation/Immunology Endocrinology
    Dagrocorat (PF-00251802) is an orally active and selective high-affinity partial agonist of the glucocorticoid receptor. Dagrocorat is also a time-dependent reversible inhibitor of CYP3A (IC50=1.3 μM in human liver microsomes) and CYP2D6 (Ki=0.57 μM in human liver microsomes). Dagrocorat can be used for the research of rheumatoid arthritis .
    Dagrocorat
  • HY-133116
    4-Hydroxyatomoxetine

    		Adrenergic Receptor Neurological Disease
    4-Hydroxyatomoxetine is an active metabolite of Atomoxetine. 4-Hydroxyatomoxetine is metabolized by the enzyme cytochrome P450 2D6 (CYP2D6). Atomoxetine hydrochloride is a potent and selective noradrenalin re-uptake inhibitor (Ki values are 5 nM, 77 nM and 1451 nM for inhibition of radioligand binding to human NET, SERT and DAT respectively) .
    4-Hydroxyatomoxetine
  • HY-RS03461
    CYP2D6 Human Pre-designed siRNA Set A

    		Small Interfering RNA (siRNA) Others

    CYP2D6 Human Pre-designed siRNA Set A contains three designed siRNAs for CYP2D6 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.

    CYP2D6 Human Pre-designed siRNA Set A
    CYP2D6 Human Pre-designed siRNA Set A
  • HY-N1483
    Guanfu base A

    		Potassium Channel Cardiovascular Disease
    Guanfu base A is an antiarrhythmic alkaloid isolated from Aconitum coreanum and is a potent noncompetitive CYP2D6 inhibitor, with a Ki of 1.20 μM in human liver microsomes (HLMs) and a Ki of 0.37 μM for the human recombinant form (rCYP2D6). Guanfu base A is also a potent competitive inhibitor of CYP2D in monkey (Ki of 0.38 μM) and dog (Ki of 2.4 μM) microsomes . Guanfu base A also inhibits HERG channel current .
    Guanfu base A
  • HY-109173
    Filapixant

    BAY 1902607

    		 P2X Receptor Cytochrome P450 Inflammation/Immunology
    Filapixant (BAY 1902607) is an orally active and selective P2X3 receptor antagonist. Filapixant is applicable to the research of refractory chronic cough .
    Filapixant
  • HY-169728
    SID 24785302

    		Hexokinase Parasite Infection
    SID 24785302 is a hexokinase inhibitor with antiparasitic activity. SID 24785302 exhibits activity against T. brucei and Leishmania. SID 24785302 can be used for the research of mitochondrial DNA disorders and parasitic infection .
    SID 24785302
  • HY-16718A
    Dagrocorat hydrochloride

    PF-00251802 hydrochloride

    		 Glucocorticoid Receptor Cytochrome P450 Inflammation/Immunology Endocrinology
    Dagrocorat (PF-00251802) hydrochloride is an orally active and selective high-affinity partial agonist of the glucocorticoid receptor. Dagrocorat hydrochloride is also a time-dependent reversible inhibitor of CYP3A (IC50=1.3 μM in human liver microsomes) and CYP2D6 (Ki=0.57 μM in human liver microsomes). Dagrocorat hydrochloride can be used for the research of rheumatoid arthritis .
    Dagrocorat hydrochloride
  • HY-15401
    WAY 163909

    		5-HT Receptor Neurological Disease Metabolic Disease
    WAY 163909 is an orally active, blood-brain barrier permeable 5-HT2C receptor-selective agonist. WAY 163909 exhibits an EC50 of 8 nM and a Ki of 10.5 nM for h5-HT2C. Instead of triggering apoptosis, WAY 163909 induces anorectic, antipsychotic-like, antidepressant-like, anti-aggressive and anti-compulsive effects. WAY 163909 alleviates ketamine-induced hypothermia, but impairs sexual function at high doses. With rapid antidepressant-like properties, WAY 163909 can be used in research related to obesity, schizophrenia, depression, obsessive-compulsive disorder, and anesthesia-induced hypothermia .
    WAY 163909
  • HY-100064R
    O-Desmethyl gefitinib (Standard)

    		Reference Standards EGFR Cancer
    O-Desmethyl gefitinib (Standard) is the analytical standard of O-Desmethyl gefitinib. This product is intended for research and analytical applications. O-Desmethyl gefitinib is an active metabolite of Gefitinib in human plasma. The formation of O-desmethyl gefitinib is dependent on CYP2D6 activity. O-desmethyl gefitinib inhibits EGFR with an IC50 of 36 nM in subcellular assays .
    O-Desmethyl gefitinib (Standard)
  • HY-N1483A
    Guanfu base A hydrochloride

    		Potassium Channel Cardiovascular Disease
    Guanfu base A hydrochloride is an antiarrhythmic alkaloid with the ability to inhibit CYP2D6 enzyme activity. Guanfu base A hydrochloride can be used to inhibit arrhythmia-related diseases. Guanfu base A hydrochloride exhibits inhibitory effects on CYP2D6 in different species of organisms, including humans, monkeys, and dogs. The biological activity of Guanfu base A hydrochloride makes it have potential clinical application value .
    Guanfu base A hydrochloride
  • HY-144285
    CXCR4 antagonist 4

    		CXCR HIV Inflammation/Immunology
    CXCR4 antagonist 4 is a potent, orally active CXCR4 antagonist (IC50=24 nM) with diminished CYP 2D6 activity, improved PAMPA permeability, potent inhibition of human immunodeficiency virus entry (IC50=7 nM) .
    CXCR4 antagonist 4
  • HY-100064S
    O-Desmethyl gefitinib-d8

    		EGFR Cancer
    O-Desmethyl gefitinib-d8 is a deuterium labeled O-Desmethyl gefitinib. O-Desmethyl gefitinib is an active metabolite of Gefitinib in human plasma. The formation of O-desmethyl gefitinib is dependent on CYP2D6 activity. O-desmethyl gefitinib inhibits EGFR with an IC50 of 36 nM in subcellular assays .
    O-Desmethyl gefitinib-d8
  • HY-100064S1
    O-Desmethyl gefitinib-d6

    		Isotope-Labeled Compounds EGFR Cancer
    O-Desmethyl gefitinib-d6 is the deuterium labeled O-Desmethyl gefitinib. O-Desmethyl gefitinib is an active metabolite of Gefitinib in human plasma. The formation of O-desmethyl gefitinib is dependent on CYP2D6 activity. O-desmethyl gefitinib inhibits EGFR with an IC50 of 36 nM in subcellular assays .
    O-Desmethyl gefitinib-d6
  • HY-144286
    CXCR4 antagonist 3

    		CXCR Infection
    CXCR4 antagonist 3 (compound 12a) is a potent antagonist of CXCR4 with an IC50 of 11 nM. CXCR4 antagonist 3 is a congener of TIQ15. CXCR4 antagonist 3 demonstrates the best overall properties including CXCR4 antagonism, CYP 2D6 inhibition, metabolic stability, and permeability. CXCR4 antagonist 3 has the potential for the research of human immunodeficiency virus .
    CXCR4 antagonist 3
  • HY-169119
    Antifungal agent 114

    		Cytochrome P450 Fungal Infection
    Antifungal agent 114 (Compound 19g) is an inhibitor for Cytochrome P450, that inhibits CYP1A2, CYP2C9, CYP2C19 CYP2D6 and CYP3A4 at 10 μM. Antifungal agent 114 exhibits antifungal activity against Cryptococcus neoformans, Candida and Aspergillus, with MIC <0.0625 μg/mL. Antifungal agent 114 exhibits good metabolic stability in human liver microsomes with a half-time of 107 minutes .
    Antifungal agent 114
  • HY-173032
    VU6033685

    		mGluR Neurological Disease
    VU6033685 is the orally active positive allosteric modulator (PAM) for mGlu1 that positively modulates human mGlu1 and human mGlu5 with EC50 of 39 nM and 3960 nM. VU6033685 also inhibits CYP1A2, CYP2C9 and CYP2D6 with IC50 of 26, 22.3 and 23.8 μM, respectively. VU6033685 reverses amphetamine-induced rats hyperlocomotion, protects rats from MK-801 (HY-15084B)-induced cognitive impairment. VU6033685 exhibits good pharmacokinetics characteristics in rats with an oral bioavailability of 42.8% .
    VU6033685
  • HY-N2129A
    N-Nornuciferine hydrochloride

    		Cytochrome P450 Cholinesterase (ChE) Neurological Disease
    N-Nornuciferine hydrochloride is an orally active, blood-brain barrier-permeable CYP2D6 inhibitor, with an IC50 of 3.76 μM and a Ki of 2.34 μM against human CYP2D6. N-Nornuciferine hydrochloride also acts as a BChE inhibitor, showing an IC50 of 5.6 μM in mice . N-Nornuciferine hydrochloride can be used in the research of neurological-related diseases .
    N-Nornuciferine hydrochloride
  • HY-10672
    Urotensin-II receptor antagonist-1

    		Urotensin Receptor Cytochrome P450 Sodium Channel Opioid Receptor Cardiovascular Disease
    Urotensin-II receptor antagonist-1 (compound 1) is a low oral bioavailability (F=0-3%, rat) selective human Urotensin II receptor antagonist, Ki=16 nM (test on HEK293 cells expressing recombinant human UT receptor). Urotensin-II receptor antagonist-1 inhibits cytochrome P450 (IC50=0.75 μM, CYP2D6; 1.4 μM, CYP3A4), inhibits κ-opioid receptor (EC50=3.2 μM), targets cardiac sodium channels (Ki=2.5 μM) .
    Urotensin-II receptor antagonist-1
  • HY-W1011921
    TDO2-IN-3

    		Indoleamine 2,3-Dioxygenase (IDO) Cancer
    TDO2-IN-3 (Compound 21) is a selective TDO2 inhibitor with an IC50 of 0.34 μM. TDO2-IN-3 can be used in cancer-related research .
    TDO2-IN-3
  • HY-183919
    ACC2-IN-1

    		Acetyl-CoA Carboxylase Cytochrome P450 Metabolic Disease
    ACC2-IN-1 is an orally active, selective inhibitor of acetyl-CoA carboxylase 2 (ACC2), with an IC50 of 1.9 nM against human targets. ACC2-IN-1 acts as a reducing agent to decrease malonyl-CoA levels in skeletal muscle and exhibits a favorable CYP450 inhibition profile. ACC2-IN-1 can be used in the research of type 2 diabetes .
    ACC2-IN-1
  • HY-182735
    BMS-570520

    		CCR Cytochrome P450 5-HT Receptor Dopamine Receptor Serotonin Transporter Inflammation/Immunology
    BMS-570520 is an orally bioavailable CCR3 antagonist with an IC50 of 1.9 nM against hCCR3 and an IC50 of 1300 nM against hCYP2D6. BMS-570520 inhibits CYP2D6, but shows low activity against off-target G protein-coupled receptors, biogenic amine transporters, and the hERG potassium channel. BMS-570520 regulates chemotaxis, calcium mobilization, and anti-inflammatory pathways. BMS-570520 can be used in research related to asthma, allergic rhinitis, and contact dermatitis .
    BMS-570520
  • HY-183763
    RORγt inverse agonist 37

    		ROR Interleukin Related Inflammation/Immunology
    RORγt inverse agonist 37 is an orally active RORγt inverse agonist with an IC50 of 10.8 nM against human targets. RORγt inverse agonist 37 destabilizes helix 12 of RORγt in the agonist-bound conformation, thereby inhibiting transcriptional activity. RORγt inverse agonist 37 inhibits the secretion of IL-17 in cells and in LPS-induced systemic inflammation mouse models. RORγt inverse agonist 37 improves disease-related symptoms in mouse models of psoriasiform dermatitis. RORγt inverse agonist 37 can be used in research related to psoriasiform dermatitis and systemic inflammation .
    RORγt inverse agonist 37
  • HY-181747
    CYP11A1-IN-3

    		Cytochrome P450 Cancer
    CYP11A1-IN-3 (Compound II-4) is a selective CYP11A1 inhibitor with an IC50 of 26.7 nM. CYP11A1-IN-3 shows selectivity towards CYP1A2, 2C9 and 2D6. CYP11A1-IN-3 can be used for the research of castration-resistant prostate cancer .
    CYP11A1-IN-3

Inquiry Online

Your information is safe with us. * Required Fields.

Salutation

  

Country or Region *

Applicant Name *

 

Organization Name *

Department *

     

Email Address *

 

Product Name *

Cat. No.

  

Requested quantity *

Phone Number *

     

Remarks

Inquiry Online

Inquiry Information

Product Name:
Cat. No.:
Quantity:
MCE Japan Authorized Agent: