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14α-Demethylase inhibitor

" in MedChemExpress (MCE) Product Catalog:

24

Inhibitors & Agonists

2

Natural
Products

4

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas Chemical Structure
  • 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-117766
    Opelconazole

    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-17514S
    Itraconazole-d5

    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-17514S1
    Itraconazole-d3

    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
    Itraconazole (Standard)

    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-W706180
    (±)-Triadimefon-d4

    		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-17514S2
    Itraconazole-d9

    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-105191
    Azalanstat

    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-14282A
    (Z)-Lanoconazole

    		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-178162
    CYP51-IN-27

    		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-169165
    14α-Demethylase-IN-1

    		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-16719
    Dapaconazole

    		Cytochrome P450 Infection
    Dapaconazole, as an antifungal agent, inhibits sterol 14α-demethylase cytochrome P450 activity with an IC50 of 1.4 μM .
    Dapaconazole
  • HY-151440
    Antifungal agent 42

    		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
    SKF 104976

    		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-151437
    Antifungal agent 40

    		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
    Antifungal agent 68

    		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-176210
    CYP51-IN-24

    		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-147777
    14α-Demethylase/DNA Gyrase-IN-2

    		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-178340
    Antifungal agent 137

    		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-147778
    14α-Demethylase/DNA Gyrase-IN-1

    		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-105191A
    Azalanstat dihydrochloride

    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-14282R
    Lanoconazole (Standard)

    		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-136755
    CYP51-IN-5

    		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

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