Ketoconazole

別名：R 41400

製品コード：S1353 純度：99.95%

Ketoconazole inhibits cyclosporine oxidase and testosterone 6 beta-hydroxylase with IC50 of 0.19 mM and 0.22 mM, respectively. Ketoconazole is an androgen biosynthesis inhibitor.

CAS No. 65277-42-1

サイズ	価格(税別)	在庫状況
10mM (1mL in DMSO)	JPY 29500	国内在庫あり
100mg	JPY 22000	国内在庫あり
1g	JPY 55500	国内在庫なし(納期7~10日)

代表番号: 045-509-1970\|電子メール：[email protected] よく尋ねられる質問

文献中Selleckの製品使用例（22）

製品安全説明書

現在のバッチを見る：純度： 99.95%

99.95

Ketoconazole関連製品

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関連化合物ライブラリー	Metabolism Compound Library Anti-cancer Metabolism Compound Library Glutamine Metabolism Compound Library Carbohydrate Metabolism Compound Library Lipid Metabolism Compound Library	もっと見る

シグナル伝達経路

P450 (e.g. CYP17)シグナル伝達経路

P450 (e.g. CYP17)阻害剤の選択性比較

Cell Data

Cell Lines	Assay Type	Incubation Time	活性情報	PMID
human THP1 cells	Cytotoxicity assay	48 h	Cytotoxicity against human THP1 cells after 48 hrs, IC50=44 μM	17960923
P815B cells	Cytotoxicity assay	24 h	Cytotoxicity against mouse P815B cells after 24 hrs by MTS/PMS assay, LD50=25 μM	25036789
LLC-PK1 epithelial cells	Function assay		Inhibition of P-glycoprotein, human L-MDR1 expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay, IC50=4.8 μM	12699389
MCF7 cells	Function assay		Inhibition of CYP26A1 in human MCF7 cells assessed as all-trans retinoic acid metabolism, IC50=12 μM	16279770
CHO cells	Function assay		Inhibition of CYP24A1 expressed in CHO cells, IC50=0.52 μM	20655626
V79 11B2 cells	Function assay		Inhibition of human CYP11B2 expressed in V79 11B2 cells, IC50=0.081 μM	16570918
V79 cells	Function assay		Inhibition of human CYP24 hydroxylase expressed in V79 cells, IC50=0.312 μM	15615534
hamster V79MZh11B1 cells	Function assay		Inhibition of human CYP11B1 expressed in hamster V79MZh11B1 cells, IC50=0.127 μM	18672868
hamster V79MZh11B2 cells	Function assay		Inhibition of human CYP11B2 expressed in hamster V79MZh11B2 cells, IC50=0.067 μM	18672868
CHO cells	Function assay		Inhibition of human ERG expressed in CHO cells by whole cell patch clamp technique, IC50=1.90546 μM	18448342
V79 11B1 cells	Function assay		Inhibition of human CYP11B1 expressed in V79 11B1 cells, IC50=0.224 μM	16570918
Topp 3 cells	Function assay		Inhibition of human CYP51 expressed in Topp 3 cells by lanosterol demethylase assay, IC50=0.19 μM	17194716
V79 cells	Function assay		Inhibition of human CYP24A1 expressed in chinese hamster V79 cells, IC50=0.312 μM	20594862
V79MZ cells	Function assay		Inhibition of human CYP11B2 expressed in hamster V79MZ cells using 11-deoxycorticosterone substrate, IC50=0.067 μM	24900247
V79MZh cells	Function assay		Inhibition of human CYP11B2 expressed in hamster V79MZh cells, IC50=0.067 μM	20550118
human epidermal keratinocytes	Function assay		Inhibition of CYP24A1 in human epidermal keratinocytes, IC50=0.126 μM	20594862
V79MZh cells	Function assay		Inhibition of human CYP11B1 expressed in hamster V79MZh cells, IC50=0.127 μM	20550118
他の多くの細胞株試験データをご覧になる場合はこちらをクリックして下さい

生物活性

製品説明

Ketoconazole inhibits cyclosporine oxidase and testosterone 6 beta-hydroxylase with IC50 of 0.19 mM and 0.22 mM, respectively. Ketoconazole is an androgen biosynthesis inhibitor.

特性

More active than both Econazole and Miconazole against Malassezia species.

Targets

Cyclosporine oxidase ^[1]	Testosterone 6 beta-hydroxylase ^[1]
0.19 mM	0.22 mM

In Vitro
In vitro	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. ^[2] 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. ^[3] Ketoconazole is susceptable to several Malassezia species with minimum inhibitory concentrations (MICs) of 0.03 µg/mL. ^[4]
Kinase Assay	Whole Cell [³H]R1881 Binding Assay
Kinase 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
細胞実験	細胞株	HT29-S-B6 colon cell
	濃度	25 μM
	反応時間	72 hours
	実験の流れ	HT29-S-B6 cells (5×10⁵) are plated in 35-mm Petri dishes. The next day, the medium is changed and effectors are added in a small volume (10-20 μL). The incubation medium is renewed every day during the experiments. The same triplicate dishes are used for cell counts, [³H]thymidine incorporation, and flow cytometry. [³H]Thymidine (0.5 μCi) is allowed to incorporate for 24 hours; at the end of incubation, cells are rinsed with 1 mL of medium, detached with 1 mL of trypsin-EDTA, and diluted (1:3) with the culture medium. An aliquot (0.5-1 mL) is used for cell count with a Coulter Counter.

In Vivo
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. ^[5] 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. ^[6]
動物実験	動物モデル	male Wistar rats
	投与量	25 mg/kg
	投与経路	Intraperitoneal injection

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
臨床試験 (data from https://clinicaltrials.gov, updated on 2024-05-22)
NCT04869449	Recruiting	Glioblastoma\|Glioblastoma Multiforme\|Glioblastoma Multiforme of Brain\|Glioblastoma Multiforme Adult	Milton S. Hershey Medical Center	May 12 2022	Early Phase 1
NCT04212000	Completed	Healthy	Cortendo AB	December 16 2019	Phase 1
NCT03796273	Recruiting	Anatomic Stage IV Breast Cancer AJCC v8\|Astrocytoma\|Breast Carcinoma Metastatic in the Brain\|Glioma\|Invasive Breast Carcinoma\|Oligodendroglioma\|Prognostic Stage IV Breast Cancer AJCC v8\|Recurrent Glioma	Wake Forest University Health Sciences\|National Cancer Institute (NCI)	March 13 2019	Early Phase 1
NCT04872920	Recruiting	Cushing Syndrome	HRA Pharma	December 20 2018	--
NCT03473418	Unknown status	Vaginal Candidiasis	Assiut University	April 1 2018	Phase 3

参考
[1] Oliver WR Jr, et al. Proc Natl Acad Sci U S A, 2001, 98(9), 5306-5311. [2] Eil C, et al. Horm Metab Res, 1992, 24(8), 367-370. [3] Forgue-Lafitte ME, et al. Cancer Res, 1992, 52(24), 6827-6831. [4] Gupta AK, et al. Br J Dermatol, 2000, 142(4), 758-765. [5] Goeders NE, et al. Drug Alcohol Depend, 1998, 53(1), 67-77. [6] Salphati L, et al. Pharmacology, 1998, 56(6), 308-313. + 展開

参考

+ 展開

化学情報

分子量	531.43	化学式	C₂₆H₂₈Cl₂N₄O₄
CAS No.	65277-42-1	SDF	Download Ketoconazole SDFをダウンロードする
Smiles	CC(=O)N1CCN(CC1)C2=CC=C(C=C2)OCC3COC(O3)(CN4C=CN=C4)C5=C(C=C(C=C5)Cl)Cl
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1年-80°Cin solvent
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	１ケ月-20°Cin solvent

In vitro
Batch:

Ethanol : 7 mg/mL

DMSO : 3 mg/mL ( (5.64 mM)；吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Water : Insoluble

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量	濃度	体積	分子量
=	×	×

希釈計算器分子量計算器

投与溶液組成計算機(クリア溶液)

ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）

投与量 mg/kg 動物平均体重 g 投与体積（動物毎）μL 動物数匹

ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

計算結果：

投与溶媒濃度： mg/ml;

DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH₂O，を加え完全に溶解させます。

投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。

注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

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