Tacrolimus (FK506)

製品コードS5003 バッチS500317

印刷

化学情報

Chemical Structure Synonyms FR900506, Fujimycin Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C44H69NO12
分子量 804.02 CAS No. 104987-11-3
Solubility (25°C)* 体外 DMSO 120 mg/mL (149.25 mM)
Ethanol 100 mg/mL (124.37 mM)
Water 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 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。

 5.000mg/ml (6.22mM) Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified 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 Tacrolimus (FK506) is a 23-membered macrolide lactone, it reduces peptidyl-prolyl isomerase activity in T cells by binding to the immunophilin FKBP12 (FK506 binding protein) creating a new complex. Tacrolimus also inhibits the phosphatase activity of calcineurin. Tacrolimus induces vascular endothelial autophagy.
in vitro

Tacrolimus (FK506) and cyclosporin A block translocation of the cytoplasmic component without affecting synthesis of the nuclear subunit in T lymphocytes. [1] It prevents T-cell proliferation by inhibiting a Ca(2+)-dependent event required for induction of interleukin-2 transcription. [2] This compound binds to distinct families of intracellular proteins (immunophilins) termed cyclophilins and FK 506-binding proteins (FKBPs). It specifically inhibits cellular calcineurin at drug concentrations that inhibit interleukin 2 production in activated T cells. [3] Tacrolimus and CsA exert nearly identical biological effects in cells by inhibiting the same subset of early calcium-associated events involved in lymphokine expression, apoptosis, and degranulation. It binds to a family of intracellular receptors termed the FK-506 binding proteins (FKBPs). [4]
in vivo

Tacrolimus (FK506) results in increase in the paw and tail withdrawal threshold as revealed by behavioral pain assessment in rats against hyperalgesic and allodynic stimuli. It also leads to a decrease in the serum nitrate and thiobarbituric acid reactive substance (TBARS) levels along with reduction in tissue myeloperoxidase (MPO) and total calcium levels, whereas, rise in tissue reduced glutathione levels in rats. This compound ameliorates the increase in the neuronal edema and axonal degeneration in rats with ischemia reperfusion (I/R). [5]

プロトコル(参考用のみ)

細胞アッセイ 細胞株 Jurkat cells
濃度 10 nM
反応時間 1 h
実験の流れ

After cells were cultured in the presence of 10 nM Tacrolimus (FK506) for 1 hr and washed, phosphatase activity was measured in lysates.
動物実験 動物モデル Male C57BL/6J mice
投薬量 30 mg/kg
投与方法 Oral

参考

  • https://pubmed.ncbi.nlm.nih.gov/1715516/
  • https://pubmed.ncbi.nlm.nih.gov/1377361/
  • https://pubmed.ncbi.nlm.nih.gov/1373887/
  • https://pubmed.ncbi.nlm.nih.gov/7509138/
  • https://pubmed.ncbi.nlm.nih.gov/20529260/
  • https://pubmed.ncbi.nlm.nih.gov/18574318/
  • https://pubmed.ncbi.nlm.nih.gov/29863266/
  • https://pubmed.ncbi.nlm.nih.gov/22130237/

カスタマーフィードバック

Data from [Biochim Biophys Acta, 2013, 1833(3), 652-62]

, 2013, Natural and Medical Sciences Institute

, 2013, Natural and Medical Sciences Institute

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：

Calcineurin governs baseline and homeostatic regulations of non-rapid eye movement sleep in mice [ Proc Natl Acad Sci U S A, 2025, 122(4):e2418317122] PubMed: 39847332
Adhesive polyelectrolyte coating through UV-triggered polymerization on PLGA particles for enhanced drug delivery to inflammatory intestinal mucosa [ J Nanobiotechnology, 2025, 23(1):32] PubMed: 39844269
Calcium-mediated mitochondrial fission and mitophagy drive glycolysis to facilitate arterivirus proliferation [ PLoS Pathog, 2025, 21(1):e1012872] PubMed: 39804926
Interferon-gamma rescues dendritic cell calcineurin-dependent responses to Aspergillus fumigatus via Stat3 to Stat1 switching [ iScience, 2025, 28(2):111535] PubMed: 39898039
Signal transduction pathways controlling Ins2 gene activity and beta cell state transitions [ iScience, 2025, 28(3):112015] PubMed: 40144638
ACSL4 Drives C5a/C5aR1-Calcium-Induced Fibroblast-to-Myofibroblast Transition in a Bleomycin-Induced Mouse Model of Pulmonary Fibrosis [ Biomolecules, 2025, 15(8)1106] PubMed: 40867551
Polymeric-Based Theranostic Nanocarriers of Neuroprotective Drugs: Development, Imaging, and Bioanalysis [ Mol Pharm, 2025, 10.1021/acs.molpharmaceut.5c00170] PubMed: 40517330
Post-Liver Transplantation Management and Specimen Collection in Daurian Ground Squirrels for Single-Cell RNA Sequencing [ J Vis Exp, 2025, (223).] PubMed: 41052099
PU.1 and BCL11B sequentially cooperate with RUNX1 to anchor mSWI/SNF to poise the T cell effector landscape [ Nat Immunol, 2024, 25(5):860-872] PubMed: 38632339
Antiviral activity of immunosuppressors alone and in combination against human adenovirus and cytomegalovirus [ Int J Antimicrob Agents, 2024, 63(5):107116] PubMed: 38401774

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。

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