Molecular Weight(MW): 531.43
Ketoconazole inhibits cyclosporine oxidase and testosterone 6 beta-hydroxylase with IC50 of 0.19 mM and 0.22 mM, respectively.
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|Description||Ketoconazole inhibits cyclosporine oxidase and testosterone 6 beta-hydroxylase with IC50 of 0.19 mM and 0.22 mM, respectively.|
|Features||More active than both Econazole and Miconazole against Malassezia species.|
Ketoconazole interacts with androgen receptors in a competitive fashion in intact human foreskin fibroblasts. Ketoconazole competes for [3H]dexamethasone binding to fibroblast glucocorticoid receptors with IC50 of 0.3 mM.  Ketoconazole reduces cell proliferation and [3H]thymidine incorporation with IC50 of 2.5 mM in the serum independent HT29-S-B6 colon cell clone. Ketoconazole inhibits the incorporation of [3H]thymidine with IC50 of 2 μM and 13 μM in the Evsa-T cell line and MDA-MB-231 cell line, respectively. Ketoconazole induces a decrease of the number of cells in S phase and a corresponding increase of the percentage of cells in Go-G1 in HT29-S-B6 cells.  Ketoconazole is susceptable to several Malassezia species with minimum inhibitory concentrations (MICs) of 0.03 µg/mL. 
|In vivo||Ketoconazole (25 mg/kg, i.p.) significantly decreases plasma corticosterone and reduces low dose cocaine self-administration without affecting food-reinforced responding in rats.  Ketoconazole raises the AUC of orally administered digoxin from 63 mg x h/L to 411 mg x h/L in rats. Ketoconazole raises the AUC of intravenously administered digoxin from 93 mg × h/L to 486 mg × h/L in rats. Ketoconazole increases digoxin bioavailability from 0.68 to 0.84 in rats, while mean absorption time is reduced from 1.1 hours to 0.3 hour. |
Whole Cell [3H]R1881 Binding Assay:Fibroblasts are grown to confluence in five or six 150 cm2 tissue culture flasks for routine assay. This usually requires 4-6 weeks from the time of the initial seeding of the cell line. All studies are performed between passages 3-20. Two days before assay, the medium is changed to one lacking fetal calf serum. This is repeated again 24 hours before assay. Competition assays are performed with 0.5-1.0 nM [3H]R1881 and increasing amounts of the nonradioactive compounds. Binding to low affinity sites is determined in the presence of 5 × 10-7 M R1881 and is subtracted from whole cell binding of [3H]R 1881 obtained in the absence of any inhibitor to assess binding to 5 high affinity site
-  Oliver WR Jr, et al. Proc Natl Acad Sci U S A, 2001, 98(9), 5306-5311.
-  Eil C, et al. Horm Metab Res, 1992, 24(8), 367-370.
-  Forgue-Lafitte ME, et al. Cancer Res, 1992, 52(24), 6827-6831.
|In vitro||Ethanol||7 mg/mL (13.17 mM)|
|DMSO||5 mg/mL warmed (9.4 mM)|
|In vivo||Add solvents individually and in order:
30% propylene glycol, 5% Tween 80, 65% D5W
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT02582177||Not yet recruiting||Tinea||Ache Laboratorios Farmaceuticos S.A.||August 2017||Phase 3|
|NCT02147964||Not yet recruiting||Gonadotropin Deficiency||University of Washington||January 2017||Phase 2|
|NCT02606383||Withdrawn||Tinea Pedis||Biolab Sanus Farmaceutica||June 2016||Phase 3|
|NCT02560051||Recruiting||Prostatic Neoplasms||The University of Texas Health Science Center, Houston||November 2015||Phase 2|
|NCT02494713||Recruiting||Prostate Cancer||The University of Texas Health Science Center, Houston||October 2015||Phase 2|
|NCT02256865||Recruiting||Insulin Resistance||Los Angeles Biomedical Research Institute||October 2014||--|
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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