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P450 1A1

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-D0092

    Cytochrome P450 Others
    7-Ethoxy-4-methylcoumarin is a coumarin derivative and can be used as a substrate probe of mammalian cytochromes P450 1A1, 2B4 and 2B6 .
    7-Ethoxy-4-methylcoumarin
  • HY-N2229
    Rhapontigenin
    2 Publications Verification

    Cytochrome P450 Fungal Bacterial Infection Inflammation/Immunology Cancer
    Rhapontigenin is a natural analog of resveratrol with anticancer, antioxidant, antifungal and antibacterial activities. Rhapontigenin is amechanism-based, potent and selective cytochrome P450 1A1 inactivator (IC50  = 400 nM). Rhapontigenin exhibits 400-fold and 23-fold selectivity for P450 1A1 over P450 1A2 and P450 1B1, respectively .
    Rhapontigenin
  • HY-131452

    Cytochrome P450 Cancer
    1-Ethynylpyrene is an aryl acetylenic inhibitor of cytochromes P450 1A1, 1A2, and 2B1 with IC50s of 0.18, 0.32, and 0.04 μM, respectively [1]. 1-Ethynylpyrene is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    1-Ethynylpyrene
  • HY-N2233
    Rhapontigenin 3'-O-glucoside
    1 Publications Verification

    Cytochrome P450 Cancer
    Rhapontigenin 3'-O-glucoside is a derivative of Rhapontigenin. Rhapontigenin is a potent inactivator of human P450 1A1 and is a good candidate for a cancer chemopreventive agent .
    Rhapontigenin 3'-O-glucoside
  • HY-Y0110

    Endogenous Metabolite Others
    2-Naphthol is a metabolite of naphthalene, catalyzed by cytochrome P450 (CYP) isozymes (CYP 1A1, CYP 1A2, CYP 2A1, CYP 2E1 and CYP 2F2).
    2-Naphthol
  • HY-117532

    PCB 118

    Pyroptosis Cancer
    PenCB (PCB 118) could induces pyroptosis by priming and activating NFκB-dependent NLRP3 inflammasome. PCB 118 induces oxidative stress and pyroptosis are dependent on Aryl hydrocarbon receptor (AhR) activation and subsequent cytochrome P450 1A1 upregulation .
    PenCB
  • HY-D0092R

    Reference Standards Cytochrome P450 Others
    7-Ethoxy-4-methylcoumarin (Standard) is the analytical standard of 7-Ethoxy-4-methylcoumarin. This product is intended for research and analytical applications. 7-Ethoxy-4-methylcoumarin is a coumarin derivative and can be used as a substrate probe of mammalian cytochromes P450 1A1, 2B4 and 2B6 .
    7-Ethoxy-4-methylcoumarin (Standard)
  • HY-N2229R

    Reference Standards Cytochrome P450 Fungal Bacterial Infection Inflammation/Immunology Cancer
    Rhapontigenin (Standard) is the analytical standard of Rhapontigenin. This product is intended for research and analytical applications. Rhapontigenin is a natural analog of resveratrol with anticancer, antioxidant, antifungal and antibacterial activities. Rhapontigenin is amechanism-based, potent and selective cytochrome P450 1A1 inactivator (IC50 = 400 nM). Rhapontigenin exhibits 400-fold and 23-fold selectivity for P450 1A1 over P450 1A2 and P450 1B1, respectively .
    Rhapontigenin (Standard)
  • HY-115824

    Cytochrome P450 Others
    7ETMC is a cytochrome P450 inhibitor with selective inhibition of human cytochrome P450s 1A1 and 1A2. 7ETMC has inhibitory effects on P450s 1A1 and 1A2 with IC?? values of 0.46μM and 0.50μM, respectively, within the first six minutes, and has no inhibitory activity against P450s 2A6 and 2B1. Except for 7-ethynyl-3-methyl-4-phenylcoumarin, the remaining inhibitors show mechanism-based inhibition of P450s 1A1 and 1A2.
    7ETMC
  • HY-N10344

    Cytochrome P450 Quinone Reductase Cancer
    Glucoarabin is a bioactive glucosinolate. In Hepa1c1c7 cells, hydrolyzed Glucoarabin (hGSL 9) upregulates the phase II detoxification enzyme quinone reductase (NQO1), with no effect on cytochrome P450 (CYP) 1A1 activity .
    Glucoarabin
  • HY-Y0110S

    Endogenous Metabolite Others
    2-Naphthol-d8 is the deuterium labeled 2-Naphthol . 2-Naphthol is a metabolite of naphthalene, catalyzed by cytochrome P450 (CYP) isozymes (CYP 1A1, CYP 1A2, CYP 2A1, CYP 2E1 and CYP 2F2) .
    2-Naphthol-d8
  • HY-Y0110S1

    Endogenous Metabolite Others
    2-Naphthol-d7 is the deuterium labeled 2-Naphthol . 2-Naphthol is a metabolite of naphthalene, catalyzed by cytochrome P450 (CYP) isozymes (CYP 1A1, CYP 1A2, CYP 2A1, CYP 2E1 and CYP 2F2) .
    2-Naphthol-d7
  • HY-Y0110R

    Reference Standards Endogenous Metabolite Others
    2-Naphthol (Standard) is the analytical standard of 2-Naphthol. This product is intended for research and analytical applications. 2-Naphthol is a metabolite of naphthalene, catalyzed by cytochrome P450 (CYP) isozymes (CYP 1A1, CYP 1A2, CYP 2A1, CYP 2E1 and CYP 2F2).
    2-Naphthol (Standard)
  • HY-117532R

    Pyroptosis Cancer
    PenCB (Standard) is the analytical standard of PenCB. This product is intended for research and analytical applications. PenCB (PCB 118) could induces pyroptosis by priming and activating NFκB-dependent NLRP3 inflammasome. PCB 118 induces oxidative stress and pyroptosis are dependent on Aryl hydrocarbon receptor (AhR) activation and subsequent cytochrome P450 1A1 upregulation .
    PenCB (Standard)
  • HY-112734

    Cytochrome P450 Cancer
    4'-Methylchrysoeriol is a potent inhibitor of Cytochrome P450 enzymes, with an IC50 of 19 nM for human P450 1B1-dependent EROD.
    4'-Methylchrysoeriol
  • HY-116050

    Cytochrome P450 Na+/K+ ATPase Cardiovascular Disease Inflammation/Immunology
    17S-HETE is arachidonic acid metabolite through cytochrome P-450 pathways. 17S-HETE serves as allosteric activator of the cytochrome P450 1B1 and inhibitor of ATPase, induces cardic hypertrophy .
    17(S)-HETE
  • HY-116196

    Na+/K+ ATPase Cytochrome P450 Cardiovascular Disease Inflammation/Immunology
    17-HETE is arachidonic acid metabolite through cytochrome P-450 pathways, which consists of 17R-HETE and 17S-HETE enantiomers. 17-HETE serves as allosteric activator of the cytochrome P450 1B1 and inhibitor of ATPase, induces cardic hypertrophy .
    17-HETE
  • HY-114955

    Cytochrome P450 Others
    MTTC is a 1,2,3-thiadiazole compound that exhibits mechanism-based inactivation, resulting in the inactivation of cytochrome P450 2E1 activity .
    MTTC
  • HY-150557

    Cytochrome P450 Cancer
    CYP1B1-IN-1 (Compound 9e) is a selective cytochrome P450 1B1 (CYP1B1) inhibitor with an IC50 of 0.49 nM .
    CYP1B1-IN-1
  • HY-152196

    Cytochrome P450 Cancer
    CYP1B1-IN-5 (Compound 6q) is a potent and selective cytochrome P450 1B1 (CYP1B1) inhibitor with an IC50 of 4.7 nM .
    CYP1B1-IN-5
  • HY-150558

    Cytochrome P450 Cancer
    CYP1B1-IN-2 (compound 9j) is a potent and selective CYP1B1 (cytochrome P450 1B1) inhibitor, with an IC50 of 0.52 nM .
    CYP1B1-IN-2
  • HY-D0145
    7-Ethoxyresorufin
    1 Publications Verification

    Resorufin ethyl ether

    Cytochrome P450 NO Synthase Others
    7-Ethoxyresorufin (Resorufin ethyl ether) is a fluorometric substrate and competitive inhibitor of cytochrome P450, especially CYP1A1. 7-Ethoxyresorufin also inhibits NO synthase .
    7-Ethoxyresorufin
  • HY-128920

    Cytochrome P450 Cancer
    Phortress free base (NSC 710305) is a P450 CYP1A1-activated antitumor prodrug with antitumor activity . Phortress free base leads to DNA damage and cell cycle arrest .
    Phortress free base
  • HY-E70468

    Cytochrome P450 Metabolic Disease
    Human CYP1A1, High-Reductase, a recombinant CYP1A1, is one of the most important cytochrome P450 (CYP) enzymes. Human CYP1A1, High-Reductase is involved in the metabolism of several genotoxic/carcinogenic environmental xenobiotics .
    Human CYP1A1,High-Reductase
  • HY-E70472

    Cytochrome P450 Metabolic Disease
    Human CYP1A1, High-Reductase, a recombinant CYP1A1, is one of the most important cytochrome P450 (CYP) enzymes. Human CYP1A1, High-Reductase is involved in the metabolism of several genotoxic/carcinogenic environmental xenobiotics .
    Human CYP1A1,Low-Reductase
  • HY-111430

    Cytochrome P450 Cancer
    1-Ethynylnaphthalene is a selective inhibitor of cytochrome P450 1B1. 1-Ethynylnaphthalene is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    1-Ethynylnaphthalene
  • HY-D0145S

    Resorufin ethyl ether-d5

    Isotope-Labeled Compounds Cytochrome P450 NO Synthase Others
    7-Ethoxyresorufin-d5 is deuterium labeled 7-Ethoxyresorufin. 7-Ethoxyresorufin (Resorufin ethyl ether) is a fluorometric substrate and competitive inhibitor of cytochrome P450, especially CYP1A1. 7-Ethoxyresorufin also inhibits NO synthase .
    7-Ethoxyresorufin-d5
  • HY-147721

    Bacterial Infection
    Dihydropteroate synthase-IN-1 (compound 5g) is a potent dihydropteroate synthase (DHPS) inhibitor. Dihydropteroate synthase-IN-1 shows antimicrobial activities and antifungal activity. Dihydropteroate synthase-IN-1 inhibits cytochromes P450. Dihydropteroate synthase-IN-1 can bu used as diagnostic radio imaging material .
    Dihydropteroate synthase-IN-1
  • HY-159006

    Cytochrome P450 Cancer
    CYP1B1 ligand 3 (Compound A1) is a selective inhibitor for cytochrome P450 enzyme CYP1B1 with an IC50 of 11.9 nM. CYP1B1 ligand 3 can be utilized for the synthesis of PROTAC CYP1B1 degrader-2 (HY-158429) .
    CYP1B1 ligand 3
  • HY-W100681R

    Drug Intermediate Reference Standards Others
    Tetrahydropiperine (Standard) is the analytical standard of Tetrahydropiperine. This product is intended for research and analytical applications. Tetrahydropiperine, a cyclohexyl analogue of piperine, is the first natural aryl pentanamide from Piper longum . Tetrahydropiperine (compound 14) inhibits the cytochrome P450 (CYP) isoform CYP1A1/arylhydrocarbon hydroxylase (AHH; IC50=23 µM) .
    2'-Hydroxy-5'-methylacetophenone (Standard)
  • HY-N4205R

    Reference Standards Cytochrome P450 Cancer
    Tetrahydropiperine (Standard) is the analytical standard of Tetrahydropiperine. This product is intended for research and analytical applications. Tetrahydropiperine, a cyclohexyl analogue of piperine, is the first natural aryl pentanamide from Piper longum . Tetrahydropiperine (compound 14) inhibits the cytochrome P450 (CYP) isoform CYP1A1/arylhydrocarbon hydroxylase (AHH; IC50=23 µM) .
    Tetrahydropiperine (Standard)
  • HY-W472509

    11-Hydroxy-5,8,12,14-eicosatetraenoic acid

    Cytochrome P450 Cardiovascular Disease
    11-HETE (11-Hydroxy-5,8,12,14-eicosatetraenoic acid) is the activator for cytochrome P450. 11-HETE upregulates the mRNA expressions of CYP1B1, CYP1A1, CYP4A11, CYP4F11, and CYP4F2, induces cell hypertrophy in RL-14 cell, and exhibits potential to be used in cardiovascular diseases .
    11-HETE
  • HY-W699866

    Isotope-Labeled Compounds PPAR Cytochrome P450 Drug Metabolite Metabolic Disease
    Gemfibrozil 1-O-β-glucuronide-d6 is the deuterium labeled Gemfibrozil 1-O-β-glucuronide (HY-129993). Gemfibrozil 1-O-β-Glucuronide, a metabolite of Gemfibrozil (CI-719; HY-B0258), is a potent and competitive P450 (CYP) isoform CYP2C8 inhibitor with an IC50 of 4.07 μM .
    Gemfibrozil 1-O-β-glucuronide-d6
  • HY-147336

    Drug Metabolite Infection Cardiovascular Disease Metabolic Disease Inflammation/Immunology
    Desmethylazelastine is a main active metabolite of Azelastine that is oxidatively metabolized by the cytochrome P450 enzyme system with a protein binding rate of 97% and an elimination half-life of 54 hours. Azelastine is an orally active, selective and high-affinity histamine H1-receptor antagonist. Azelastine can be used in studies of allergic rhinitis, asthma, diabetic hyperlipidemic and SARS-CoV-2 .
    Desmethylazelastine
  • HY-147999

    Bacterial Fungal Cytochrome P450 Infection
    GlcN-6-P Synthase-IN-1 (Compound 4d) is a Glucosamine-6-phosphate (GlcN-6-P) synthase inhibitor with an IC50 of 3.47 μM. GlcN-6-P Synthase-IN-1 exhibits significant antimicrobial activity. GlcN-6-P Synthase-IN-1 has good penetration in the CNS and is able to inhibit the cytochrome P450, CYP3A4 isoform .
    GlcN-6-P Synthase-IN-1
  • HY-121888

    PPAR Metabolic Disease
    20-HEPE is a metabolite of eicosapentaenoic acid formed by ω-oxidation of EPA by cytochrome P450 (CYP) ω-oxidases, including human CYP4F3B. At 10 μM, it activates peroxisome proliferator-activated receptor α (PPARα) in COS-7 cells expressing a luciferase reporter gene. 20-HEPE also activates mouse transient receptor potential vanilloid receptor 1 (mTRPV1) in vitro but lacks analgesic activity in rats.
    20-HEPE
  • HY-160431

    PPAR Metabolic Disease
    8(9)-EET is a major cytochrome P450 (CYP450) metabolite in the renal cortex [1][2]. It activates PPARα in HEK293 cells when used at a concentration of 1 μM but inhibits NF-κB activity induced by IL-1β in a PPARα-dependent and -independent fashion . It is also a substrate of COX-1 and COX-2, as measured by oxygen consumption and product formation assays when used at a concentration of 50 μM .
    8(9)-EET
  • HY-108347
    CP-100356 hydrochloride
    Maximum Cited Publications
    8 Publications Verification

    P-glycoprotein BCRP Metabolic Disease
    CP-100356 hydrochloride is an orally active dual MDR1 (P-gp)/BCRP inhibitor, with an IC50s of 0.5 and 1.5 µM for inhibiting MDR1-mediated Calcein-AM transport and BCRP-mediated Prazosin transport, respectively. CP-100356 hydrochloride is also a weak inhibitor of OATP1B1 (IC50=∼66 µM). CP-100356 hydrochloride is devoid of inhibition against MRP2 and major human P450 enzymes (IC50>15 µM) .
    CP-100356 hydrochloride
  • HY-10965

    KW-3902

    Adenosine Receptor Neurological Disease
    Rolofylline (KW-3902) is a potent, selective adenosine A1 receptor antagonist that is under development for the treatment of patients with acute congestive heart failure and renal impairment. Rolofylline is metabolized primarily to the pharmacologically active M1-trans and M1-cis metabolites by cytochrome P450 (CYP450) . Rolofylline is alleviating the presynaptic dysfunction and restores neuronal activity as well as dendritic spine levels in vitro, is an interesting candidate to combat the hypometabolism and neuronal dysfunction associated with Tau-induced neurodegenerative diseases .
    Rolofylline
  • HY-146393
    PROTAC CYP1B1 degrader-1
    1 Publications Verification

    PROTACs Cytochrome P450 Cancer
    PROTAC CYP1B1 degrader-1 (Compound 6C), a α-naphthoflavone chimera derivative, is able to eliminate cytochrome P450 (CYP)1B1-mediated agent resistance via targeted CYP1B1 degradation, with IC50s of 95.1 and 9838.6 nM for CYP1B1 and CYP1A2, respectively. PROTAC CYP1B1 degrader-1 can be used for the research of CYP1B1-overexpressing prostate cancer .
    PROTAC CYP1B1 degrader-1
  • HY-161649

    Cytochrome P450 Aryl Hydrocarbon Receptor Cancer
    hCYP1B1-IN-2 (compound 3n) is a potent human cytochrome P450 1B1 enzyme hCYP1B1 inhibitor. hCYP1B1-IN-2 shows the extremely potent anti-hCYP1B1 activity (IC50=0.040 nM) and blocks AhR transcription activity. hCYP1B1-IN-2 potently inhibits hCYP1B1 via a mix inhibition manner, showing a Ki value of 21.71 pM .
    hCYP1B1-IN-2
  • HY-10965R

    Adenosine Receptor Neurological Disease
    Rolofylline (Standard) is the analytical standard of Rolofylline. This product is intended for research and analytical applications. Rolofylline (KW-3902) is a potent, selective adenosine A1 receptor antagonist that is under development for the treatment of patients with acute congestive heart failure and renal impairment. Rolofylline is metabolized primarily to the pharmacologically active M1-trans and M1-cis metabolites by cytochrome P450 (CYP450) . Rolofylline is alleviating the presynaptic dysfunction and restores neuronal activity as well as dendritic spine levels in vitro, is an interesting candidate to combat the hypometabolism and neuronal dysfunction associated with Tau-induced neurodegenerative diseases .
    Rolofylline (Standard)
  • HY-B0822S1

    GABA Receptor Cytochrome P450 Inflammation/Immunology
    Fipronil- 13C6 is the 13C-labeled Fipronil. Fipronil is an insecticide that acts as a selective antagonist of insect GABA receptors (IC50s = 30 nM and 1,600 nM for cockroach and rat receptors, respectively). Fipronil also inhibits desensitizing and non-desensitizing glutamate-induced chloride currents in cockroach neurons (IC50s = 800 nM and 10 nM, respectively). Fipronil induces activity of the cytochrome P450 (CYP) isoforms CYP1A1/2, CYP2B1/2, and CYP3A1/2 in isolated rat liver microsomes.
    Fipronil-13C6
  • HY-10672

    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-W072025

    Cytochrome P450 Keap1-Nrf2 Heme Oxygenase (HO) Reactive Oxygen Species (ROS) Inflammation/Immunology
    CYP2E1-IN-1 (Compound 10) is an orally active cytochrome P450 2E1 (CYP2E1) inhibitor with a Kd of 7.02 μM, an IC50 of 1.64 μM, and a Ki of 0.897 μM. CYP2E1-IN-1 activates the Nrf2/HO-1 signaling pathway and inhibits ROS production, thereby alleviating pancreatic injury. CYP2E1-IN-1 has significant anti-inflammatory and antioxidant activities and can effectively reduce inflammation and oxidative stress in severe acute pancreatitis (SAP). CYP2E1-IN-1 can be used in the study of SAP and other inflammatory-related diseases .
    CYP2E1-IN-1
  • HY-W762015

    1,2,3,6,7,8-HxCDF

    Cytochrome P450 Cancer
    1,2,3,6,7,8-Hexachlorodibenzofuran (1,2,3,6,7,8-HxCDF) is a dioxin-like polychlorinated dibenzofuran (PCDF). 1,2,3,6,7,8-Hexachlorodibenzofuran induces expression of the genes encoding aryl hydrocarbon hydroxylase (AHH) and ethoxyresorufin-O-deethylase (EROD) in H-4-II-E rat hepatoma cells (EC50s = 1.47 and 1.24 nM, respectively). 1,2,3,6,7,8-Hexachlorodibenzofuran reduces weight, induces thymic atrophy, and induces the expression of genes encoding the cytochrome P450 (CYP) isoform CYP1A1 and 4-chlorobiphenyl hydroxylase in rats (EC50s = 3.2, 0.9, 0.35, and 0.21 µmol/kg, respectively) .
    1,2,3,6,7,8-Hexachlorodibenzofuran

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