14α-demethylase

Itraconazole (R51211) is a triazole antifungal agent that inhibits cytochrome P-450-dependent enzymes necessary for ERGOSTEROL synthesis.

14α-Demethylase-IN-1 (compound 2e) is an inhibitor of 14α-demethylase and serves as an antifungal agent. For Candida albicans, Candida parapsilosis, Candida krusei, and Candida glabrata, the MIC50 values recorded at 48 hours are 2.47 μM, 1.23 μM, 19.70 μM, and 19.70 μM respectively.

14α-Demethylase/DNA Gyrase-IN-2 (Compound 6a) is a potent inhibitor of 14α-Demethylase and DNA Gyrase, exhibiting significant antibacterial activity.

14α-Demethylase/DNA Gyrase-IN-1 (Compound 7c) is a potent inhibitor of 14α-Demethylase/DNA Gyrase, exhibiting antibacterial activity.

PC945 (Opelconazole) is a potent broad-spectrum antifungal compound with inhibitory effect on fumonisinol 14α-demethylase (CYP51A/CYP51B), which can be used in the study of fungal infections of the lungs.

Ketoconazole (R-41400) is an imidazole antifungal agent with broad-spectrum antifungal activity that primarily acts by inhibiting the biosynthesis of ergosterol in the fungal cell membrane. Ketoconazole inhibits the fungal cytochrome P450-dependent enzyme lanosterol 14α-demethylase (CYP51), thereby blocking the conversion of lanosterol to ergosterol. This leads to damage to the cell membrane structure and permeability, consequently inhibiting fungal growth and producing an antifungal effect. In addition, ketoconazole is a non-selective cytochrome P450 (CYP) inhibitor, specifically inhibiting drug-metabolizing enzymes such as human CYP3A4. In terms of endocrinology, ketoconazole also inhibits various enzymes involved in steroid synthesis (CYP17A1, CYP11A1).

(Rac)-Ketoconazole ((Rac)-R 41400) is an orally active antifungal imidazole compound. It inhibits ergosterol synthesis in fungi by targeting the cytochrome P450-dependent enzyme, 14α-sterol demethylase (CYP51), on the fungal cell membrane. This disruption leads to dysfunction of the cell membrane, ultimately hindering fungal growth and proliferation. (Rac)-Ketoconazole is applicable in studying fungal infections.

CYP51-IN-24 (Compound 22) is an inhibitor of Sterol 14α-Demethylase (CYP51). It exhibits potent inhibitory activity against both wild-type and resistant fungi. By binding to the fungal CYP51 enzyme, CYP51-IN-24 prevents the biosynthesis of ergosterol. This compound is applicable in the research and development of treatments for drug-resistant fungal infections.

Antifungalagent 136 (Compound M-15) is an irreversible inhibitor of fungal lanosterol 14α-demethylase (CYP51). It exhibits potent antifungal activity against drug-resistant Candida albicans and can downregulate the expression of IL-6. Antifungalagent 136 shows promise for research into fungal infections and inflammatory diseases.

CYP51-IN-27 is an inhibitor of sterol 14α-demethylase CYP51 with an IC50 of 0.3434 μg/mL. It exhibits antifungal activity by inhibiting the production of fungal ergosterol. CYP51-IN-27 is applicable in infection-related research, such as studies on rice sheath blight.

Antifungalagent 137 (Compound 4S) is an antifungal compound that inhibits Phomopsis sp. (PS) with an EC50 value of 0.15 μg/mL. It targets lanosterol 14α-demethylase (CYP51) with an IC50 value of 5.00 μg/mL. Additionally, it disrupts PS mycelial morphology, compromises cell membrane integrity, and increases intracellular ROS levels, inducing oxidative stress. This compound is useful for research on fungal infections.

Antifungal agent 40 inhibits C. alb. CYP51 lanosterol 14α-demethylase (CYP51) by extending into the narrow hydrophobic pocket II, thereby affecting biofilm formation.

Antifungal agent 42 is an antifungal compound that inhibits biofilm formation and targets C.alb.'s lanosterol 14α-demethylase (CYP51).

Pyrisoxazole is a novel fungicide inhibitor of Sterol 14α-demethylase.

Azalanstat HCl is an anti-obesity drug acting as a lanosterol 14α-demethylase inhibitor. Azalanstat HCl has been shown to inhibit cholesterol synthesis in HepG2 cells, human fibroblasts, hamster hepatocytes and hamster liver, by inhibiting the cytochrome P450 enzyme lanosterol 14 alpha-demethylase. When administered orally to hamsters fed regular chow, RS-21607 (50 mg/kg/day) lowered serum cholesterol in a dose-dependent manner (ED50 = 62 mg/kg) in a period of 1 week. It preferentially lowered low density lipoprotein (LDL) cholesterol and apo B relative to high density lipoprotein (HDL) cholesterol and apo A-1.

Azalanstat mesylate is an anti-obesity drug acting as a lanosterol 14α-demethylase inhibitor. Azalanstat mesylate has been shown to inhibit cholesterol synthesis in HepG2 cells, human fibroblasts, hamster hepatocytes and hamster liver, by inhibiting the cytochrome P450 enzyme lanosterol 14 alpha-demethylase. When administered orally to hamsters fed regular chow, RS-21607 (50 mg/kg/day) lowered serum cholesterol in a dose-dependent manner (ED50 = 62 mg/kg) in a period of 1 week. It preferentially lowered low density lipoprotein (LDL) cholesterol and apo B relative to high density lipoprotein (HDL) cholesterol and apo A-1.

Antifungal agent 68 (compound 10) effectively combats fungal infections caused by Candida and Cryptococcus gattii through the inhibition of ergosterol biosynthesis, likely via interaction with lanosterol 14α-demethylase (CYP51). The imidazole ring of antifungal agent 68 is proposed to interact with the heme group of CYP51 [1].

Itraconazole-D9 is the deuterated form of Itraconazole. Itraconazole (T1011) (R51211) is a triazole antifungal agent with potent oral activity as a Hedgehog signaling pathway antagonist, exhibiting an IC50 of approximately 800 nM. It effectively inhibits lanosterol 14α-demethylase (Cytochrome P450), thus preventing the conversion of lanosterol to ergosterol. Additionally, Itraconazole (T1011) exhibits anti-cancer and anti-angiogenic properties and acts as an oxysterol-binding protein (OSBP) inhibitor.

Pyrisoxazole (Standard) is the standard substance of Pyrisoxazole, and it is applicable for quantitative analysis, quality control, and related research in biochemical experiments. Pyrisoxazole is a novel fungicide inhibitor of Sterol 14α-demethylase.