Ketoconazole
Chemical Name: cis-1-Acetyl-4-[4-[[2-(2,4-dichlorophenyl)-2-(1H-imidazol-1-ylmethyl)-1,3-dioxolan-4-yl] methoxy]phenyl]piperazine
Purity: ≥99%
Biological Activity
Ketoconazole is an inhibitor of cytochrome P450c17. Enhances the formation of myelin basic protein-positive oligodendrocytes from oligodendrocyte progenitor cells in vitro and promotes remyelination in vivo. Also an antifungal agent. Brain penetrant.Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Background References
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High-throughput genotoxicity assay identifies antioxidants as inducers of DNA damage response and cell death.
Fox JT, Sakamuru S, Huang R
Proc. Natl. Acad. Sci. U.S.A., 2012;109(14):5423-8. -
Accumulation of 8,9-unsaturated sterols drives oligodendrocyte formation and remyelination.
Hubler et al.
Nature, 2018;560:372 -
Induction of myelinating oligodendrocytes in human cortical spheroids.
Madhavan et al.
Nat.Methods., 2018;15:700 -
Inhibition of human adrenal steroidogenic enzymes in vitro by imidazole drugs including ketoconazole.
Ayub and Levell
J.Steroid Biochem., 1989;32:515 -
Blockade of HERG and Kv1.5 by ketoconazole.
Dumaine et al.
J.Pharmacol.Exp.Ther., 1998;286:727 -
Ketoconazole inhibition of the bifunctional cytochrome P450c17 does not affect androgen formation from the endogenous lyase substrate.
Kuhn-Velten et al.
Biochem.Pharmacol., 1992;44:2371
Product Datasheets
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Citations for Ketoconazole
The citations listed below are publications that use Tocris products. Selected citations for Ketoconazole include:
4 Citations: Showing 1 - 4
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Inhibition of proliferation and migration of melanoma cells by ketoconazole and Ganoderma immunomodulatory proteins.
Authors: Lu Et al.
Oncol Lett 2019;18:891
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Central activation of TRPV1 and TRPA1 by novel endogenous agonists contributes to mechanical allodynia and thermal hyperalgesia after burn injury.
Authors: Green Et al.
Mol Pain 2016;12
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Role of endogenous TRPV1 agonists in a postburn pain model of partial-thickness injury.
Authors: Green Et al.
Pain 2013;154:2512
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The cytochrome P450 inhibitor, ketoconazole, inhibits oxidized linoleic acid metabolite-mediated peripheral inflammatory pain.
Authors: Ruparel Et al.
Mol Pain 2012;8:73
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