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14α-Demethylase

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製品番号 製品名 Target 研究分野 構造式
  • HY-17514
    Itraconazole
    20+ Cited Publications

    R51211

    Fungal Hedgehog Cytochrome P450 Autophagy Antibiotic Bacterial Infection Cancer
    Itraconazole (R51211) is a triazole antifungal agent and a potent and orally active Hedgehog (Hh) signaling pathway antagonist with an IC50 of ~800 nM. Itraconazole potently inhibits lanosterol 14α-demethylase (cytochrome P450 enzyme), thereby inhibits the oxidative conversion of lanosterol to ergosterol. Itraconazole has anticancer and antiangiogenic effects. Itraconazole is a oxysterol-binding protein (OSBP) inhibitor .
    Itraconazole
  • HY-134124

    Reactive Oxygen Species (ROS) Metabolic Disease
    Glutathione ethyl ester is a cell-permeable GSH donor and provides an efficient supply of GSH to the oocyte. Glutathione ethyl ester shows positive effect on the in vitro production of embryos by enhancement of the antioxidative defense .
    Glutathione ethyl ester
  • HY-P10272

    PTG-300

    Ferroportin Others
    Rusfertide is a peptide mimetic of natural hepcidin, which targets and degrades ferroportin, reduces serum iron and transferrin-saturation, and thus regulates the production of red blood cells. Rusfertide ameliorates the polycythemia vera, β-thalassemia and hereditary hemochromatosis .
    Rusfertide
  • HY-A0248A
    Polymyxin B1
    1 Publications Verification

    Bacterial Infection
    Polymyxin B1 is a potent antimicrobial lipopeptide first derived from Bacilus polymyxa. Polymyxin B1 is the major component in Polymyxin B (HY-A0248). Polymyxin B1 can induce lysis of bacterial cells through interaction with their membranes. Polymyxin B1 has the potential for multidrug-resistant Gram-negative bacterial infections treatment .
    Polymyxin B1
  • HY-117766

    PC945

    Fungal Cytochrome P450 Infection
    Opelconazole (PC945), a potent, long-acting antifungal triazole, possesses activity against a broad range of both azole-susceptible and azole-resistant strains of Aspergillus fumigatus. Opelconazole is also a potent, tightly binding inhibitor of A. fumigatus sterol 14α-demethylase activity, CYP51A and CYP51B, with IC50s of 0.23 μM and 0.22 μM, respectively .
    Opelconazole
  • HY-P1108A
    Astressin 2B TFA
    1 Publications Verification

    CRFR Neurological Disease Inflammation/Immunology
    Astressin 2B TFA is a blood-brain barrier-impermeable, highly selective CRFR2 antagonist (rCRFR2, IC50=0.57 nM). Astressin 2B TFA blocks the protective effects mediated by CRFR2, thereby exacerbating indomethacin (HY-14397)-induced hemorrhagic intestinal injury in rats. Astressin 2B TFA reverses the protective effects of Urocortin 1 against intestinal hypermotility, bacterial invasion and upregulation of inflammatory mediators. Astressin 2B TFA also blocks the anxiogenic effect of Urocortin 2 and attenuates stress-induced anxiety-related behaviors. In the Clostridioides difficile toxin A (C. difficile toxin A)-mediated enteritis model, Astressin 2B TFA mimics the phenotype of CRFR2-deficient mice, significantly exacerbating intestinal epithelial damage, edema, neutrophil migration and the expression of multiple proinflammatory cytokines. Astressin 2B TFA is an important tool molecule for investigating the intestinal protective mechanisms of CRFR2 .
    Astressin 2B TFA
  • HY-P1108
    Astressin 2B
    1 Publications Verification

    CRFR Neurological Disease Inflammation/Immunology
    Astressin 2B is a blood-brain barrier-impermeable, highly selective CRFR2 antagonist (rCRFR2, IC50=0.57 nM). Astressin 2B blocks the protective effects mediated by CRFR2, thereby exacerbating indomethacin (HY-14397)-induced hemorrhagic intestinal injury in rats. Astressin 2B reverses the protective effects of Urocortin 1 against intestinal hypermotility, bacterial invasion and upregulation of inflammatory mediators. Astressin 2B also blocks the anxiogenic effect of Urocortin 2 and attenuates stress-induced anxiety-related behaviors. In the Clostridioides difficile toxin A (C. difficile toxin A)-mediated enteritis model, Astressin 2B mimics the phenotype of CRFR2-deficient mice, significantly exacerbating intestinal epithelial damage, edema, neutrophil migration and the expression of multiple proinflammatory cytokines. Astressin 2B is an important tool molecule for investigating the intestinal protective mechanisms of CRFR2 .
    Astressin 2B
  • HY-17514S

    R51211-d5

    Fungal Hedgehog Cytochrome P450 Autophagy Antibiotic Infection Cancer
    Itraconazole-d5 is the deuterium labeled Itraconazole. Itraconazole (R51211) is a triazole antifungal agent and a potent and orally active Hedgehog (Hh) signaling pathway antagonist with an IC50 of ~800 nM. Itraconazole potently inhibits lanosterol 14α-demethylase (cytochrome P450 enzyme), thereby inhibits the oxidative conversion of lanosterol to ergosterol. Itraconazole has anticancer and antiangiogenic effects .
    Itraconazole-d5
  • HY-14282
    Lanoconazole
    1 Publications Verification

    Fungal Infection Inflammation/Immunology
    Lanoconazole is a potent and orally active imidazole antifungal agent, shows a broad spectrum of activity against fungi?in vitro?and?in vivo . Lanoconazole interferes with ergosterol biosynthesis by inhibiting sterol 14-alpha demethylase and blocking fungal membrane ergosterol biosynthesis. Lanoconazole can be used for the investigation of dermatophytosis and onychomycosis .
    Lanoconazole
  • HY-B2012

    DPX-H6573

    Environmental Pollutants Fungal Infection
    Flusilazole (DPX-H6573) is a broad-spectrum fungicide and cytochrome P-450 inhibitor that can be used in studies related to fungal infections .
    Flusilazole
  • HY-17514S1

    R51211-d3

    Antibiotic Autophagy Bacterial Cytochrome P450 Fungal Hedgehog Infection Cancer
    Itraconazole-d3 (R51211-d3) is the deuterium labeled Itraconazole (HY-17514) . Itraconazole (R51211) is a triazole antifungal agent and a potent and orally active Hedgehog (Hh) signaling pathway antagonist with an IC50 of ~800 nM. Itraconazole potently inhibits lanosterol 14α-demethylase (cytochrome P450 enzyme), thereby inhibits the oxidative conversion of lanosterol to ergosterol. Itraconazole has anticancer and antiangiogenic effects. Itraconazole is a oxysterol-binding protein (OSBP) inhibitor.
    Itraconazole-d3
  • HY-17514R

    R51211 (Standard)

    Reference Standards Fungal Hedgehog Cytochrome P450 Autophagy Antibiotic Bacterial Infection Cancer
    Itraconazole (Standard) is the analytical standard of Itraconazole. This product is intended for research and analytical applications. Itraconazole (R51211) is a triazole antifungal agent and a potent and orally active Hedgehog (Hh) signaling pathway antagonist with an IC50 of ~800 nM. Itraconazole potently inhibits lanosterol 14α-demethylase (cytochrome P450 enzyme), thereby inhibits the oxidative conversion of lanosterol to ergosterol. Itraconazole has anticancer and antiangiogenic effects. Itraconazole is a oxysterol-binding protein (OSBP) inhibitor .
    Itraconazole (Standard)
  • HY-P10143

    Ac-Pro-Leu-Gly-[(S)-2-mercapto-4-methyl-pentanoyl]-Leu-Gly-OEt

    MMP Others
    MMP-2/MMP-9 Substrate (Ac-Pro-Leu-Gly-[(S)-2-mercapto-4-methyl-pentanoyl]-Leu-Gly-OEt) is a synthetic chromogenic polypeptide substrate whose core structure mimics the cleavage sites of MMP-2 and MMP-9 (gelatinase A and B) in collagen. After being hydrolyzed by collagenase, MMP-2/MMP-9 Substrate reacts with 4,4'-dithiodipyridine or Ellman's Reagent via its thiol fragment to produce a product with ultraviolet absorption properties .
    MMP-2/MMP-9 Substrate
  • HY-A0248AS

    Isotope-Labeled Compounds Bacterial Infection
    Polymyxin B1-d7 TFA is the deuterium labeled Polymyxin B1 TFA (HY-A0248A). Polymyxin B1 is a potent antimicrobial lipopeptide first derived from Bacilus polymyxa. Polymyxin B1 is the major component in Polymyxin B (HY-A0248). Polymyxin B1 can induce lysis of bacterial cells through interaction with their membranes. Polymyxin B1 has the potential for multidrug-resistant Gram-negative bacterial infections treatment .
    Polymyxin B1-d7 TFA
  • HY-W706180

    Isotope-Labeled Compounds Fungal Infection
    (±)-Triadimefon-d4 is deuterium labeled Triadimefon. Triadimefon is a triazole fungicide used to control powdery mildew, rusts, and other fungal pests on grains, fruit and vegetable crops, turf, shrubs, and trees. Triadimefon inhibits lanosterol 14α-demethylase, interfering with oxidative demethylation reactions in the ergosterol biosynthesis pathway of fungi, and also blocks gibberellin biosynthesis .
    (±)-Triadimefon-d4
  • HY-P10563

    BHV-1100

    CD38 Cancer
    Noraramtide (BHV-1100) is an antibody recruitment molecule. Noraramtide can specifically bind to CD38 molecules to recruit natural killer (NK) cells. Noraramtide enhances the ability of NK cells to kill tumor cells through antibody-dependent cellular cytotoxicity (ADCC). This mechanism allows NK cells to more effectively recognize and eliminate tumor cells while avoiding mutual killing between NK cells. Noraramtide can be used for the study of autologous cancer immunity .
    Noraramtide
  • HY-17514S2

    R51211-d9

    Fungal Hedgehog Bacterial Autophagy Cytochrome P450 Antibiotic Infection
    Itraconazole-d9 is the deuterium labeled Itraconazole . Itraconazole (R51211) is a triazole antifungal agent and a potent and orally active Hedgehog (Hh) signaling pathway antagonist with an IC50 of ~800 nM. Itraconazole potently inhibits lanosterol 14α-demethylase (cytochrome P450 enzyme), thereby inhibits the oxidative conversion of lanosterol to ergosterol. Itraconazole has anticancer and antiangiogenic effects. Itraconazole is a oxysterol-binding protein (OSBP) inhibitor .
    Itraconazole-d9
  • HY-169165

    Fungal Infection
    14α-Demethylase-IN-1 (compound 2e) is a 14α-demethylase inhibitor and can be used as an antifungal agent. 14α-Demethylase-IN-1 (48 h) exhibits MIC50 values of 2.47 μM, 1.23 μM, 19.70 μM, and 19.70 μM for C. albicans, C. parapsilosis, C. krusei, and C. glabrata, respectively .
    14α-Demethylase-IN-1
  • HY-14282A

    Fungal Infection Inflammation/Immunology
    (Z)-Lanoconazole is the Z configuration of Lanoconazole. Lanoconazole is a potent and orally active imidazole antifungal agent, shows a broad spectrum of activity against fungi in vitro and in vivo . Lanoconazole interferes with ergosterol biosynthesis by inhibiting sterol 14-alpha demethylase and blocking fungal membrane ergosterol biosynthesis. Lanoconazole can be used for the investigation of dermatophytosis and onychomycosis .
    (Z)-Lanoconazole
  • HY-105191

    RS-21607

    Cytochrome P450 Reactive Oxygen Species (ROS) Metabolic Disease
    Azalanstat (RS-21607) is an inhibitor of heme oxygenase and lanosterol 14α-demethylase, with inhibitory activity against HO-1 (IC50 = 5.5 µM) and HO-2 (IC50 = 24.5 µM). Azalanstat reduces the maturation rate of rat oocytes, increases rat oocyte degeneration, and partially inhibits progesterone production in preovulatory follicles of rats .
    Azalanstat
  • HY-147777

    Bacterial DNA/RNA Synthesis Infection
    14α-Demethylase/DNA Gyrase-IN-2 (Compound 6a) is a potent inhibitor of 14α-Demethylase/DNA Gyrase. 14α-Demethylase/DNA Gyrase-IN-2 has antimicrobial activities .
    14α-Demethylase/DNA Gyrase-IN-2
  • HY-147778

    Bacterial DNA/RNA Synthesis Infection
    14α-Demethylase/DNA Gyrase-IN-1 (Compound 7c) is a potent inhibitor of 14α-Demethylase/DNA Gyrase. 14α-Demethylase/DNA Gyrase-IN-1 has antimicrobial activities .
    14α-Demethylase/DNA Gyrase-IN-1
  • HY-P3066

    d(CH2)5Tyr(Et)VAVP

    Vasopressin Receptor Metabolic Disease
    SKF 100398 (d(CH2)5Tyr(Et)VAVP), an arginine vasopressin (AVP) analogue, is a specific antagonist of the antidiuretic effect of exogenous and endogenous AVP .
    SKF 100398
  • HY-178162

    Fungal Cytochrome P450 Infection
    CYP51-IN-27 is a sterol 14α-demethylase CYP51 inhibitor with an IC50 of 0.3434 μg/mL. CYP51-IN-27 exhibits antifungal activity and inhibits the production of fungal ergosterol. CYP51-IN-27 can be used for the research of infection, such as rice sheath blight .
    CYP51-IN-27
  • HY-W264454

    Bacterial Infection
    Antibacterial agent 303 (compound 3) is an antibacterial agent exhibiting potent antibacterial activity against MDR strains, with MICs of 10 and 100 µg/mL against Pseudomonas aeruginosa MDR1 and Staphylococcus aureus MDR strains, respectively. Antibacterial agent 303 displays strong binding affinities to E. coli DNA gyrase and Candida albicans lanosterol 14α-demethylase. Antibacterial agent 303 can be used for drug-resistant infections research .
    Antibacterial agent 303
  • HY-16719

    Cytochrome P450 Infection
    Dapaconazole, as an antifungal agent, inhibits sterol 14α-demethylase cytochrome P450 activity with an IC50 of 1.4 μM .
    Dapaconazole
  • HY-P10828

    Virus Protease Infection Inflammation/Immunology
    MAPI is a polypeptide irreversible 3C cysteine protease (SV3CP) inhibitor. MAPI inhibits SV3CP by covalently binding its C-terminal Michael-acceptor extension to the active site thiol of SV3CP Cys 139. MAPI is promising for research of noroviruses infection .
    MAPI
  • HY-151440

    Fungal Infection
    Antifungal agent 42 is an antifungal agent. Antifungal agent 42 has an inhibitory effect on lanosterol 14α-demethylase (CYP51) of C.alb.. Antifungal agent 42 inhibits biofilm formation .
    Antifungal agent 42
  • HY-117219

    Cytochrome P450 HMG-CoA Reductase (HMGCR) Endogenous Metabolite Metabolic Disease
    SKF 104976 is a 3,2-carboxylic acid derivative with potent 14-alpha-demethylase (14 alpha DM) inhibitory activity. SKF 104976 inhibited 14 alpha DM activity by 50% at 2 nM in Hep G2 cell extracts. SKF 104976 inhibited the incorporation of [14C]acetate into cholesterol in intact cells at similar concentrations, accompanied by accumulation of lanosterol, and resulted in a 40-70% decrease in 3-hydroxy-3-methylglutaryl-CoA reductase (HMGR) activity. SKF 104976 did not affect the uptake and degradation of low-density lipoprotein in Hep G2 cells, indicating that HMGR and low-density lipoprotein receptor activities are not coordinately regulated under these conditions. The inhibitory effect of SKF 104976 on HMGR activity remained unchanged even when the flux of carbon units in the sterol synthesis pathway was reduced by 80%. SKF 104976 did not inhibit HMGR activity under conditions where sterol synthesis was almost completely blocked by lovastatin .
    SKF 104976
  • HY-10445

    Azoline; R126638

    Fungal Infection
    Pramiconazole is a broad-spectrum antifungal agent with oral activity. Pramiconazole has a good affinity for 14α-demethylase. Pramiconazole can be used in the study of fungal infections in the local skin, hair, nails, oral cavity, and genital mucosa .
    Pramiconazole
  • HY-151437

    Fungal Infection
    Antifungal agent 40 is an antifungal agent which extends into the narrow hydrophobic pocket II of C.alb. CYP51. Antifungal agent 40 has an inhibitory effect on lanosterol 14α-demethylase (CYP51). Antifungal agent 40 inhibits biofilm formation .
    Antifungal agent 40
  • HY-155710

    Fungal Infection
    Antifungal agent 68 (compound 10) is an antifungal agent against Candida and Cryptococcus gattii. Antifungal agent 68 inhibits fungal ergosterol biosynthesis, possibly by targeting lanosterol 14α-demethylase (CYP51). There is an interaction between the imidazole ring of antifungal agent 68 and the heme group of CYP51 .
    Antifungal agent 68
  • HY-147919

    Fungal Infection
    Antifungal agent 33 (compound 4e) is a potent antifungal agent. Antifungal agent 33 exhibits remarkable antifungal activity against C. albicans, with a MIC of 16 μg/mL. Antifungal agent 33 shows potent inhibitory activity against Lanosterol 14α-demethylase (CYP51), with an IC50 of 0.19 μg/mL .
    Antifungal agent 33
  • HY-W414596

    Fungal Infection
    Metconazole is a 14α-demethylation inhibitor (DMI) fungicide. Metconazole inhibits fungal ergosterol biosynthesis, inhibits mycelial growth and conidial germ tube elongation. Metconazole reduces antioxidant enzyme activities. Metconazole reduces occurrence of Fusarium crown rot in wheat .
    Metconazole
  • HY-176210

    Fungal Cytochrome P450 Infection
    CYP51-IN-24 (Compound 22) is a Sterol 14α-Demethylase (CYP51) inhibitor. CYP51-IN-24 exhibits potent inhibitory activity against wild-type and drug-resistant fungi. CYP51-IN-24 inhibits ergosterol biosynthesis by binding to the fungal CYP51 enzyme. CYP51-IN-24 can be used in research and drug development against drug-resistant fungal infections .
    CYP51-IN-24
  • HY-178340

    Cytochrome P450 Fungal Reactive Oxygen Species (ROS) Infection
    Antifungal agent 137 (Compound 4S) is an antifungal agent. Antifungal agent 137 inhibits Phomopsis sp. (PS), with an EC50 of 0.15 μg/mL. Antifungal agent 137 inhibits lanosterol 14α-demethylase (CYP51), with an IC50 of 5.00 μg/mL. Antifungal agent 137 disrupts the morphology of PS mycelia, impairs cell membrane integrity, and induces an increase in intracellular ROS levels, triggering oxidative stress. Antifungal agent 137 can be used for the study of fungal infection .
    Antifungal agent 137
  • HY-14282R

    Reference Standards Fungal Infection Inflammation/Immunology
    Lanoconazole (Standard) is the analytical standard of Lanoconazole. This product is intended for research and analytical applications. Lanoconazole is a potent and orally active imidazole antifungal agent, shows a broad spectrum of activity against fungi in vitro and in vivo . Lanoconazole interferes with ergosterol biosynthesis by inhibiting sterol 14-alpha demethylase and blocking fungal membrane ergosterol biosynthesis. Lanoconazole can be used for the investigation of dermatophytosis and onychomycosis .
    Lanoconazole (Standard)
  • HY-105191A

    RS-21607 dihydrochloride

    Heme Oxygenase (HO) Metabolic Disease
    Azalanstat dihydrochloride (RS-21607 dihydrochloride) is an inhibitor of heme oxygenase and lanosterol 14α-demethylase, with inhibitory activity against HO-1 (IC50 = 5.5 µM) and HO-2 (IC50 = 24.5 µM). Azalanstat dihydrochloride reduces the maturation rate of rat oocytes, increases rat oocyte degeneration, and partially inhibits progesterone production in preovulatory follicles of rats .
    Azalanstat dihydrochloride
  • HY-P2592

    Cholecystokinin Receptor Others
    Ro 23-7014 is an appetite suppressant. Ro 23-7014 is an analog of cholecystokinin (CCK-7) .
    Ro 23-7014
  • HY-125628

    Endogenous Metabolite Infection
    Kahalalide A is an anti-mycobacterial compound with antimicrobial activity. Kahalalide A is derived from the marine mollusk Elysia rufescens. Kahalalide A has attracted extensive attention in natural product research due to its potential medicinal value .
    Kahalalide A
  • HY-136755

    Cytochrome P450 Fungal Infection
    CYP51-IN-5 is a cytochrome P450 14α-demethylase (CYP51) inhibitor and an antifungal (fungal) agent belonging to the triazole derivative class. CYP51-IN-5 is applicable to the research of Candida albicans, Cryptococcus neoformans, Candida parapsilosis, Candida tropicalis, Trichophyton rubrum, Candida krusei and Microsporum gypseum .
    CYP51-IN-5
  • HY-183091

    Fungal Infection
    Antifungal agent 159 is an antifungal agent with broad-spectrum activity against phytopathogenic fungi. Antifungal agent 159 binds tightly to the active sites of exo-β-(1,3)-glucanase, topoisomerase II-DNA-nucleotide, dihydrofolate reductase, sterol 14-α demethylase and chitin synthase. Antifungal agent 159 can be used in studies related to phytopathogenic fungal infections .
    Antifungal agent 159
  • HY-A0248AS1

    Isotope-Labeled Compounds Bacterial Infection
    Polymyxin B1-D-Leu-d7 TFA is the deuterium labeled Polymyxin B1 (HY-A0248A). Polymyxin B1 is a potent antimicrobial lipopeptide first derived from Bacilus polymyxa. Polymyxin B1 is the major component in Polymyxin B (HY-A0248). Polymyxin B1 can induce lysis of bacterial cells through interaction with their membranes. Polymyxin B1 has the potential for multidrug-resistant Gram-negative bacterial infections treatment .
    Polymyxin B1-D-Leu-d7 TFA
  • HY-181511

    Cytochrome P450 Fungal Infection
    CYP51-IN-32 is an antifungal agent with an IC50 of 0.331 μM against CYP51 of Candida albicans. CYP51-IN-32 releases hydrogen sulfide (H2S) and inhibits hyphal formation and biofilm development of Candida albicans. CYP51-IN-32 can be formulated into PEG-based nanovesicles. CYP51-IN-32 is applicable to the research of Candida albicans infection .
    CYP51-IN-32
  • HY-W281071

    Fungal Infection
    Antifungal agent 150 is an antifungal agent with activity against phytopathogenic fungi and in planta lesion suppression. Antifungal agent 150 inhibits ergosterol biosynthesis via targeted enzyme interaction. Antifungal agent 150 can be used for the research of plant diseases caused by Rhizoctonia solani, including banded leaf and sheath blight of maize .
    Antifungal agent 150

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