Clofazimine

製品コードS4107 バッチS410702

印刷

化学情報

Chemical Structure Synonyms NSC-141046 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C27H22Cl2N4
分子量 473.4 CAS No. 2030-63-9
Solubility (25°C)* 体外 DMSO 5 mg/mL (10.56 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。

 0.15mg/ml (0.32mM) Taking the 1 mL working solution as an example, add 50 μL of 3 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。

 0.15mg/ml (0.32mM) Taking the 1 mL working solution as an example, add 50 μL of 3 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 Clofazimine (NSC-141046) is a rhimophenazine dye, originally developed for the treatment of tuberculosis, it has both antimicrobial and antiinflammatory activity, postulated mechanisms of action include intercalation of clofazimine with bacterial DNA and increasing levels of cellular phospholipase A2.
in vitro Clofazimine stimulates oxygen consumption and superoxide generation by neutrophils, this compound also causes phospholipase A2 activation in neutrophils, resulting in increased release of lysophosphatidylcholine and arachidonic acid from neutrophil membranes. It inhibits mitogen-induced stimulation of peripheral blood mononuclear cells. This chemical stabilizes lysosomal membranes in macrophages and inhibits Mycobacterium leprae metabolism in mouse peritoneal macrophages. [1] It (5 mg/mL) causes dose-related enhancement of the activity of phospholipase A2 in S. aureus, according to an increase in the release of 3H-radiolabeled arachidonate and lysophosphatidylethanolamine ([3H]LPE) from bacterial-membrane phospholipids. [2] This compound inhibits 90% of twenty M. tuberculosis strains with MICs <1.0 μg/mL, to be noted, it inhibits M. tuberculosis strain 2227 with MICs of 0.06 μg/mL. It (1 μg/mL) dose-dependently inhibits activity of J774A.1 macrophages. [3]
in vivo Clofazimine (20 mg/kg) prevents mortality and causes a significant reduction in the numbers of CFU in the lungs and spleens of C57BL/6 mice infected M.tuberculosis H37Rv. [3] Liposomal Clofazimine (L-CLF) (50 mg/kg) dose-dependently reduces CFU 2 to 3 log units in the spleen, liver, and lungs of acutely infected mice with Mycobacterium tuberculosis Erdman. [4] This compound (500 μg, bid) results in highest Clofazimine concentrations in spleens and livers of mice whereas Clofazimine concentrations in the lungs are significantly lower. This chemical (20 mg/kg) is effective in reducing bacterial loads in the liver, spleen and lungs of C57BL/6 mice experimentally infected with M. avium strain TMC 724. [5]
特徴 Intracellular activities of Clofazimine are superior to that of B4154.

プロトコル(参考用のみ)

参考

  • https://pubmed.ncbi.nlm.nih.gov/7829710/
  • https://pubmed.ncbi.nlm.nih.gov/1482140/
  • https://pubmed.ncbi.nlm.nih.gov/8851584/
  • https://pubmed.ncbi.nlm.nih.gov/10390215/
  • https://pubmed.ncbi.nlm.nih.gov/10629016/

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：

The Dual-Targeted Fusion Inhibitor Clofazimine Binds to the S2 Segment of the SARS-CoV-2 Spike Protein [ Viruses, 2024, 16(4)640] PubMed: 38675980
RECOVER identifies synergistic drug combinations in vitro through sequential model optimization [ Cell Rep Methods, 2023, 3(10):100599] PubMed: 37797618
Deregulation and epigenetic modification of BCL2-family genes cause resistance to venetoclax in hematologic malignancies [ Blood, 2022, blood.2021014304] PubMed: 35704690
Activity of Drug Combinations against Mycobacterium abscessus Grown in Aerobic and Hypoxic Conditions [ Microorganisms, 2022, 10(7)1421] PubMed: 35889140
High-Throughput Screening of an FDA-Approved Drug Library Identifies Inhibitors against Arenaviruses and SARS-CoV-2 [ ACS Infect Dis, 2020, acsinfecdis.0c00486] PubMed: 33183004
Drug repositioning as a therapeutic strategy for neurodegenerations associated with OPA1 mutations [ Hum Mol Genet, 2020, ddaa244] PubMed: 33231680

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。