Acetazolamide

製品コードS4506 バッチS450603

印刷

化学情報

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

C4H6N4O3S2

分子量 222.25 CAS No. 59-66-5
Solubility (25°C)* 体外 DMSO 44 mg/mL (197.97 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.
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O

この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。

2.200mg/ml (9.90mM) Taking the 1 mL working solution as an example, add 50 μL of 44 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
Clear solution
5% DMSO 95% Corn oil

この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。

0.730mg/ml (3.28mM) Taking the 1 mL working solution as an example, add 50 μL of 14.6 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
* <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 Acetazolamide (Diamox), a potent carbonic anhydrase (CA) inhibitor, is commonly used in clinical practice as an immediate and readily available option for acute reduction of intraocular pressure(IOP).
in vitro acetazolamide reduces invasiveness of cancer cells in vitro[3].
in vivo Acetazolamide reduces inflammation-induced heat hyperalgesia, probably acting both peripherally and centrally[1]. This compound shows significant inhibitory effect on angiogenesis in CAM and endothelial cell proliferation[2]. It is clinically used to reduce intraocular pressure in glaucoma, to correct metabolic alkalosis, and to manage cerebral edema. Its treatment may also be beneficial as an adjunct to cancer chemotherapy, because it can produce additive tumor growth delays with anticancer drugs in vivo[3].

プロトコル(参考用のみ)

細胞アッセイ 細胞株 renal carcinoma cell lines(Caki-1, Caki-2, ACHN, and A-498)
濃度 10 μM
反応時間 48 h
実験の流れ

The invasion assay is performed in a Biocoat Matrigel invasion chamber. Cells (n = 1.8 × 105) are added to the chamber and cultured for 48 h in the presence or absence of acetazolamide, which was administered twice during the 48-h period: the first dose at the beginning of the assay and the second after 24 h. After growing for 48 h, noninvasive cells are removed from the upper surface of the membrane with a cotton swab. The invasive cells on the lower surface of the membrane are fixed with 4% (vol/vol) neutral-buffered formaldehyde, stained with toluidine blue, and counted in 20 separate areas with a Leitz Diaplan microscope.

動物実験 動物モデル Male Sprague-Dawley rats
投薬量 10, 100, 200 mg/kg
投与方法 i.p.

参考

  • https://pubmed.ncbi.nlm.nih.gov/15743922/
  • https://pubmed.ncbi.nlm.nih.gov/15169637/
  • https://pubmed.ncbi.nlm.nih.gov/10688890/
  • http://accessmedicine.mhmedical.com/book.aspx?bookid=374

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:

Carbonic anhydrase 2-derived drug-responsive domain regulates membrane-bound cytokine expression and function in engineered T cells [ Commun Biol, 2025, 8(1):28] PubMed: 39789216
Alterations in gene expression associated with invasion of RAS-mutant thyroid tumors and their potential diagnostic and therapeutic utility [ Eur Thyroid J, 2025, 14(3)e250022] PubMed: 40440326
Novel energy optimizer, meldonium, rapidly restores acute hypobaric hypoxia-induced brain injury by targeting phosphoglycerate kinase 1 [ Cell Commun Signal, 2024, 22(1):383] PubMed: 39075489
Carbonic anhydrase inhibitor alleviates retinal barrier toxicity in paclitaxel-induced retinopathy and macular edema by inhibiting CAXIV [ Int Ophthalmol, 2024, 44(1):437] PubMed: 39578251
Eleutheroside B ameliorated high altitude pulmonary edema by attenuating ferroptosis and necroptosis through Nrf2-antioxidant response signaling [ Biomed Pharmacother, 2022, 156:113982] PubMed: 36411652
The carbonic anhydrase inhibitor acetazolamide inhibits urinary bladder cancers via suppression of β-catenin signaling [ Cancer Sci, 2022, 113(8):2642-2653] PubMed: 35723039
Meldonium Ameliorates Hypoxia-Induced Lung Injury and Oxidative Stress by Regulating Platelet-Type Phosphofructokinase-Mediated Glycolysis [ Front Pharmacol, 2022, 13:863451] PubMed: 35450040
Effect of cGMP-activated aquaporin 1 on TRPV4 in rats with allodynia induced by chronic compression of the dorsal root ganglion. [ Neurosci Lett, 2019, 10.1016/j.neulet.2019.134630] PubMed: 31790718

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。