Ketoconazole

Manufactured by Cayman Chemical

Sourced in United States

Ketoconazole is a synthetic antifungal agent used in laboratory research. It functions as an inhibitor of the cytochrome P450 enzyme system, which is involved in the biosynthesis of sterols, including ergosterol, a critical component of fungal cell membranes.

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Lab products found in correlation

6 protocols using ketoconazole

In Vitro Enzymatic Characterization

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Sepin-1 (2,2-dimethyl-5-nitro-2H-benzimidazole-1,3-dioxide) with >97% purity was purchased from ChemBridge (San Diego, CA, United States). Phenacetin, efavirenz, paclitaxel, (S)-mephenytoin, quercetin, α-naphthoflavone, ticlopidine, ketoconazole, sulfaphenazole, and dextromethorphan were purchased from Cayman Chemical (Ann Arbor, MI, United States). Reduced GSH, diclofenac sodium, quinidine, midazolam solution, formic acid, and NADPH were obtained from Sigma-Aldrich (St. Louis, MO, United States). HLM, MLM, and RLM, and the recombinant human CYP450s (EasyCYP Bactosomes) were purchased from XenoTech (Lenexa, KS, United States). All the solvents for LC and MS were of the highest grade commercially available.

Li F., Zhang N., Gorantla S., Gilbertson S.R, & Pati D. (2018). The Metabolism of Separase Inhibitor Sepin-1 in Human, Mouse, and Rat Liver Microsomes. Frontiers in Pharmacology, 9, 313.

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In Vitro Inhibition Profiling

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DLX, [(3S)-N-methyl-3-(1-naphthyloxy)-3-(2-thienyl)propan-1-amine)], alpha-naphthoflavone (α-NF), nootkatone (NK), quercetin (QT), ticlopidine (TCP), ketoconazole, (KCZ), and sulfaphenazole (SPA) were purchased from Cayman Chemical (Ann Arbor, MI). Quinidine (Quin), formic acid, and NADPH were obtained from Sigma-Aldrich (St. Louis, MO). HLM (XTreme 200 Mixed Gender Human Liver Microsomes), MLM (Mouse Liver Microsomes), and the recombinant human CYP450s (EasyCYP Bactosomes) were purchased from XenoTech (Lenexa, KS). All solvents for liquid chromatography and mass spectrometry (LC-MS) were of the highest grade commercially available.

Qin X., Hakenjos J.M., MacKenzie K.R., Barzi M., Chavan H., Nyshadham P., Wang J., Jung S.Y., Guner J.Z., Chen S., Guo L., Krishnamurthy P., Bissig K.D., Palmer S., Matzuk M.M, & Li F. (2022). Metabolism of a Selective Serotonin and Norepinephrine Reuptake Inhibitor Duloxetine in Liver Microsomes and Mice. Drug Metabolism and Disposition, 50(2), 128-139.

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Cholesterol and Lipid Modulation

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The following reagents were purchased from Cayman Chemicals - u18666A (cat #10009085), ketoconazole (cat #15212), Filipin III (cat #70440), NileRed (cat # 30787). Gemcitabine (cat #G6423) and cholesterol (cat #C8667-1G) were purchased from Sigma.

Ondari E., Wilkins A., Latimer B., Dragoi A.M, & Ivanov S.S. (2022). Cellular cholesterol licenses Legionella pneumophila intracellular replication in macrophages. Microbial Cell, 10(1), 1-17.

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Evaluation of Drug Metabolism Kinetics

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Chlorzoxazone
(purity ≥ 98%), propranolol hydrochloride (purity ≥
99%), verapamil hydrochloride (purity ≥ 99%), ranitidine hydrochloride
(purity ≥ 98%), procaine (purity ≥ 97%), ammonium formate
(MS grade), phosphate buffer saline (PBS), and NADPH were procured
from Sigma-Aldrich. HLMs (lot no# PLO5OC-E) and MLMs (lot no# MS046-C)
were obtained from Gibco. Paracetamol (purity ≥ 98%) and ketoconazole
(purity ≥ 98%) were acquired from Cayman. Acetonitrile and
methanol (MS grade) were purchased from Thermo Fisher Scientific.
All other experimental materials were of bioreagent grade or above.
Ultrapure water was obtained from the water purification unit (Direct-Q3,
Merck-Millipore).

Manhas D., Gour A., Bhardwaj N., Sharma D.K., Sharma K., Vij B., Jain S.K., Singh G, & Nandi U. (2021). Pharmacokinetic Assessment of Rottlerin from Mallotus philippensis Using a Highly Sensitive Liquid Chromatography–Tandem Mass Spectrometry-Based Bioanalytical Method. ACS Omega, 6(48), 32637-32646.

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Substrate Specificity of Efflux Pumps

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The following compounds listed from smallest to largest (molecular weights in bracket) were used to determine the substrate specificity of the two possible efflux pumps: anisomycin (ANI; 265), acridine orange (AOR; 265), cycloheximide (CHX; 281), terbinafine (TRB; 291), trichodermin (TRD; 292), FLC (306; Diflucan; Pfizer Laboratories, Auckland, New Zealand), clotrimazole (CLT; 345; Bayer, Osaka, Japan), VRC (349; Cayman Chemical, MI, United States), difenoconazole (DFC; 406), rhodamine 6G (R6G; 479), ketoconazole (KTC; 531) and nigericin (NIG; 725). ANI, AOR, CHX, TRB, TRD, DFC, R6G, KTC, and NIG were purchased from Sigma-Aldrich, MO, United States. To test the drug susceptibilities of cells, 10 mL YPD overnight cultures of yeast cells were diluted 1:20 into 3 mL complete supplement mixture (CSM) pH 7.0 (0.69% YNB, 2% glucose, 0.079% CSM, 10 mM MOPS, 20 mM HEPES; pH 7.0) and grown to mid-logarithmic growth phase (OD₆₀₀ ∼1; ∼10⁷ cells/mL) at 30°C for ∼4 h. Broth microdilution assays of twofold serial dilutions of test compounds in CSM pH 7.0 were used to determine the minimum growth inhibitory concentrations (MIC) of test compounds. The MIC was defined as the lowest concentration of drug that inhibited growth by >90% (Niimi et al., 2004 (link)).

James J.E., Lamping E., Santhanam J, & Cannon R.D. (2021). PDR Transporter ABC1 Is Involved in the Innate Azole Resistance of the Human Fungal Pathogen Fusarium keratoplasticum. Frontiers in Microbiology, 12, 673206.

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CYP Inhibition Assay Protocol

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Williams’ Medium E, perhexiline maleate salt (racemic mixture), quinidine, β-nicotinamide adenine dinucleotide 2′-phosphate reduced tetrasodium salt hydrate (NADPH), formic acid, and dimethysulfoxide (DMSO) were purchased from Sigma-Aldrich (St. Louis, MO). Cis-OH-Phx and trans-OH-Phx were purchased from Toronto Research Chemicals (Toronto, Canada), and no information is available on the enantiomeric and diastereomeric composition of these standards. α-Naphthoflavone, nootkatone, and ketoconazole were obtained from Cayman Chemical (Ann Arbor, MI). Xtreme 200-donor Mixed Gender Human Liver Microsomes and EasyCYP bactosomes (recombinant human CYPs) were purchased from XenoTech (Lenexa, KS). Antibiotic–antimycotic was obtained from Life Technologies (Carlsbad, CA). PureCol^® Type I Collagen Solution was from Advanced BioMatrix (San Diego, CA). Fetal Bovine Serum (FBS) was purchased from Atlanta Biologicals (Lawrenceville, GA). All solvents for liquid chromatography and mass spectrometry were of the highest grade commercially available.

Nimura K., Takahashi H, & Yoshikawa H. (2001). Characterization of the dnaK Multigene Family in the Cyanobacterium Synechococcus sp. Strain PCC7942. Journal of Bacteriology, 183(4), 1320-1328.

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