Itraconazole

別名:R 51211

Itraconazole is a relatively potent inhibitor of CYP3A4 with IC50 of 6.1 nM, used as a triazole antifungal agent. Itraconazole is a potent antagonist of the Hedgehog (Hh) signaling pathway. Itraconazole suppresses the growth of glioblastoma through induction of autophagy.

Itraconazole化学構造

CAS No. 84625-61-6

サイズ 価格(税別) 在庫状況
JPY 37000 国内在庫あり
JPY 85500 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(40)

製品安全説明書

現在のバッチを見る: S247606 DMSO] 35 mg/mL] true] Water] Insoluble] false] Ethanol] Insoluble] false 純度: 99.88%
99.88

Itraconazole関連製品

Hedgehog/Smoothened阻害剤の選択性比較

Cell Data

Cell Lines Assay Type Concentration Incubation Time 活性情報 PMID
human HUVEC cells Function assay 2 μM 24 h Inhibition of VEGFR2 glycosylation in human HUVEC cells at 2 uM after 24 hrs by Western blot analysis 21936514
human HTLA cells Function assay 20 mins Inhibition of CX3CL1-stimulated CX3CR1 in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay, IC50=0.1 μM 23437772
human PBMC Cytotoxicity assay 72 h Cytotoxicity against human PBMC assessed as cell viability after 72 hrs by MTT assay, IC50=1.53 μM 24485783
human hepatocytes Function assay Inhibition of CYP3A4 in human hepatocytes using testosterone as substrate by HPLC/MS/MS method, IC50=0.07 μM 24948565
LLC-PK1 epithelial cells Function assay Inhibition of P-glycoprotein, mouse L-mdr1a expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay, IC50=0.2 μM 12699389
Topp 3 cells Function assay Inhibition of human CYP51 expressed in Topp 3 cells by lanosterol demethylase assay, IC50=3.6 μM 17194716
human MRC5 cells Cytotoxicity assay Cytotoxicity against human MRC5 cells, CC50=49.33 μM 20805398
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生物活性

製品説明 Itraconazole is a relatively potent inhibitor of CYP3A4 with IC50 of 6.1 nM, used as a triazole antifungal agent. Itraconazole is a potent antagonist of the Hedgehog (Hh) signaling pathway. Itraconazole suppresses the growth of glioblastoma through induction of autophagy.
Targets
CYP3A4 [6]
(human liver microsomes)
6.1 nM
In Vitro
In vitro Itraconazole is metabolized into hydroxy-itraconazole (OH-ITZ), a known in vivo metabolite of ITZ, and two new metabolites: keto-itraconazole (keto-ITZ) and N-desalkyl-itraconazole (ND-ITZ). Itraconazole is a substrate for CYP3A in vitro and to characterize the metabolites generated. Itraconazole exhibits an unbound Km of 3.9 nM for CYP3A. Itraconazole metabolites are as potent as or more potent CYP3A4 inhibitors than ITZ itself. [1] Itraconazole appears to act on the essential Hh pathway component Smoothened (SMO) by a mechanism distinct from that of cyclopamine and other known SMO antagonists, and prevents the ciliary accumulation of SMO normally caused by Hh stimulation. [2] Itraconazole is active against 60 clinical isolates of Aspergillus spp. with geometric mean (GM) MICs of 0.25 mg/mL. [3] Itraconazole acts primarily by impairing the synthesis of ergosterol, resulting in a defective fungal cell membrane with altered permeability and function. Itraconazole is effective for a wide variety of mycotic infections and some fungal meningeal infections. [4] Itraconazole has an affinity for mammalian cytochrome P-450 enzymes as well as for fungal P-450-dependent enzyme, and thus has the potential for clinically important interactions (e.g., astemizole, terfenadine, rifampin, oral contraceptives, H2 receptor antagonists, warfarin, cyclosporine). [5]
実験結果図 Methods Biomarkers 結果図 PMID
Western blot pACC / ACC / p-S6K / S6K GLI1 / GLI2 / p-AKT1 / AKT1 / Cyclin D1 28103683
Growth inhibition assay Cell viability 24905460
In Vivo
In Vivo Itraconazole, like other Hh pathway antagonists, can suppress Hh pathway activity and the growth of medulloblastoma in a mouse allograft model. [2]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05563766 Not yet recruiting
Esophageal Adenocarcinoma|Esophageal Squamous Cell Carcinoma|Gastroesophageal Junction Carcinoma
VA Office of Research and Development|Durham VA Health Care System|VA Palo Alto Health Care System|Portland VA Medical Center|VA Puget Sound Health Care System|Michael E. DeBakey VA Medical Center|VA Boston Healthcare System
May 1 2024 Phase 2
NCT06357520 Recruiting
Healthy Participants
AstraZeneca
April 16 2024 Phase 1
NCT06348888 Recruiting
Advanced Non-small Cell Lung Cancer|EGFR Mutation|HER2 Mutation|Healthy Volunteers
Bayer
April 10 2024 Phase 1
NCT06362642 Recruiting
Healthy Volunteers
PMV Pharmaceuticals Inc
March 28 2024 Phase 1

化学情報

分子量 705.65031 化学式

C35H38Cl2N8O4

CAS No. 84625-61-6 SDF Download Itraconazole SDFをダウンロードする
Smiles CCC(C)N1C(=O)N(C=N1)C2=CC=C(C=C2)N3CCN(CC3)C4=CC=C(C=C4)OCC5COC(O5)(CN6C=NC=N6)C7=C(C=C(C=C7)Cl)Cl
保管

In vitro
Batch:

DMSO : 35 mg/mL ( (49.59 mM); Warmed with 50℃ water bath; Ultrasonicated; 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

Ethanol : 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

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)

mg/kg g μL

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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Handling Instructions

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よくある質問(FAQ)

質問1:
We are finding the best vehicle to administer Itraconazole to mice. We want a mild vehicle (unlike DMSO) which resembles water, PBS, saline (for i.p/ injection) or methyl cellulose (for oral).

回答
We are not able to dissolve S2476 Itraconazole clearly without DMSO. For oral gavage, this compound can be dissolved in 1% CMC Na at 20mg/ml as a homogeneous suspension.

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