Itraconazole

製品コードS2476 バッチS247605

印刷

化学情報

Chemical Structure Synonyms R 51211 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C35H38Cl2N8O4
分子量 705.65031 CAS No. 84625-61-6
Solubility (25°C)* 体外 DMSO (warmed with 50ºC water bath) 13 mg/mL (18.42 mM)
Water Insoluble
Ethanol Insoluble
体内 （毎回新しく調製した物を用意してください）
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
* <1 mg/ml means slightly soluble or insoluble.
* 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.

溶剤液（一定の濃度）を調合する

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.
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). This compound is a substrate for CYP3A in vitro and to characterize the metabolites generated. It exhibits an unbound Km of 3.9 nM for CYP3A. Its metabolites are as potent as or more potent CYP3A4 inhibitors than ITZ itself. [1] This compound 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] It is active against 60 clinical isolates of Aspergillus spp. with geometric mean (GM) MICs of 0.25 mg/mL. [3] It acts primarily by impairing the synthesis of ergosterol, resulting in a defective fungal cell membrane with altered permeability and function. This chemical is effective for a wide variety of mycotic infections and some fungal meningeal infections. [4] It 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]
in vivo Itraconazole, like other Hh pathway antagonists, can suppress Hh pathway activity and the growth of medulloblastoma in a mouse allograft model. [2]

プロトコル(参考用のみ)

参考

  • https://pubmed.ncbi.nlm.nih.gov/15242978/
  • https://pubmed.ncbi.nlm.nih.gov/20385363/
  • https://pubmed.ncbi.nlm.nih.gov/9145880/
  • https://pubmed.ncbi.nlm.nih.gov/8083506/
  • https://pubmed.ncbi.nlm.nih.gov/9594936/
  • https://pubmed.ncbi.nlm.nih.gov/15242978/

カスタマーフィードバック

, , PLoS One, 2014, 9(10):e109487.

Data from [Data independently produced by , , Cancer Lett, 2017, 385:128-136]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

EGFR TKIs suppress MUC1 glycosylation through the PI3K/AKT/SP1/C1GALT1 pathway to enhance TnMUC1 CAR-T efficacy in EGFR-mutant NSCLC [ Cell Rep Med, 2025, S2666-3791(25)00272-1] PubMed: 40562040
Pyrvinium Pamoate Synergizes with Azoles in vitro and in vivo to Exert Antifungal Efficacy Against Candida auris and Other Candida Species [ Infect Drug Resist, 2025, 18:783-789] PubMed: 39958982
Experimental and network pharmacology certify itraconazole mitigates fluorouracil-induced intestinal damage by inhibiting mTOR-mediated intestinal senescence [ Toxicol Appl Pharmacol, 2025, 502:117404] PubMed: 40449753
Patient-derived rhabdomyosarcoma cells recapitulate the genetic and transcriptomic landscapes of primary tumors [ iScience, 2024, 27(10):110862] PubMed: 39319271
Improved Broad Spectrum Antifungal Drug Synergies with Cryptomycin, a Cdc50-Inspired Antifungal Peptide [ ACS Infect Dis, 2024, 10(11):3973-3993] PubMed: 39475550
Synergistic activity of the combination of falcarindiol and itraconazole in vitro against dermatophytes [ Front Cell Infect Microbiol, 2023, 13:1128000] PubMed: 37207188
Interactions between antifungals and everolimus against Cryptococcus neoformans [ Front Cell Infect Microbiol, 2023, 13:1131641] PubMed: 37026056
The Synergistic Effect of Tacrolimus (FK506) or Everolimus and Azoles Against Scedosporium and Lomentospora Species In Vivo and In Vitro [ Front Cell Infect Microbiol, 2022, 12:864912] PubMed: 35493742
Synergistic effect of pyrvinium pamoate and posaconazole against Cryptococcus neoformans in vitro and in vivo [ Front Cell Infect Microbiol, 2022, 12:1074903] PubMed: 36569209
The Antineoplastic Effect of Carboplatin Is Potentiated by Combination with Pitavastatin or Metformin in a Chemoresistant High-Grade Serous Carcinoma Cell Line [ Int J Mol Sci, 2022, 24(1)97] PubMed: 36613537

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。