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Synonyms | FR900506, Fujimycin | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C44H69NO12 |
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分子量 | 804.02 | CAS No. | 104987-11-3 | |
Solubility (25°C)* | 体外 | DMSO | 100 mg/mL (124.37 mM) | |
Ethanol | 100 mg/mL (124.37 mM) | |||
Water | Insoluble | |||
* <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. |
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. |
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in vitro | FK-506 and cyclosporin A block translocation of the cytoplasmic component without affecting synthesis of the nuclear subunit in T lymphocytes. [1] FK-506 prevents T-cell proliferation by inhibiting a Ca(2+)-dependent event required for induction of interleukin-2 transcription. [2] FK 506 binds to distinct families of intracellular proteins (immunophilins) termed cyclophilins and FK 506-binding proteins (FKBPs). FK-506 specifically inhibits cellular calcineurin at drug concentrations that inhibit interleukin 2 production in activated T cells. [3] FK-506 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. FK-506 binds to a family of intracellular receptors termed the FK-506 binding proteins (FKBPs). [4] |
in vivo | FK-506 results in increase in the paw and tail withdrawal threshold as revealed by behavioral pain assessment in rats against hyperalgesic and allodynic stimuli. FK-506 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. FK-506 ameliorates the increase in the neuronal edema and axonal degeneration in rats with ischemia reperfusion (I/R). [5] |
細胞アッセイ | 細胞株 | Jurkat cells |
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濃度 | 10 nM | |
反応時間 | 1 h | |
実験の流れ | Cells were cultured in the presence of 10 nM FK 506 for 1 hr and washed, and phosphatase activity was measured in lysates. |
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動物実験 | 動物モデル | Male C57BL/6J mice |
投薬量 | 30 mg/kg | |
投与方法 | Oral |
Data from [Biochim Biophys Acta, 2013, 1833(3), 652-62]
, 2013, Natural and Medical Sciences Institute
, 2013, Natural and Medical Sciences Institute
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 |
The mTOR pathway controls phosphorylation of BRAF at T401 [ Cell Commun Signal, 2024, 22(1):428] | PubMed: 39223665 |
Calcineurin inhibitor effects on kidney electrolyte handling and blood pressure: tacrolimus versus voclosporin [ Nephrol Dial Transplant, 2024, gfae119] | PubMed: 38777623 |
FOXO1 promotes cancer cell growth through MDM2-mediated p53 degradation [ J Biol Chem, 2024, 300(4):107209] | PubMed: 38519029 |
Calcineurin-dependent contributions to fitness in the opportunistic pathogen Candida glabrata [ mSphere, 2024, 9(1):e0055423] | PubMed: 38171022 |
(S)-(-)-blebbistatin O-benzoate has the potential to improve atopic dermatitis symptoms in NC/Nga mice by upregulating epidermal barrier function and inhibiting type 2 alarmin cytokine induction [ PLoS One, 2024, 19(5):e0302781] | PubMed: 38713650 |
(S)-(-)-blebbistatin O-benzoate has the potential to improve atopic dermatitis symptoms in NC/Nga mice by upregulating epidermal barrier function and inhibiting type 2 alarmin cytokine induction [ PLoS One, 2024, 19(5):e0302781] | PubMed: 38713650 |
Akap5 links synaptic dysfunction to neuroinflammatory signaling in a mouse model of infantile neuronal ceroid lipofuscinosis [ Front Synaptic Neurosci, 2024, 16:1384625] | PubMed: 38798824 |
Growth patterns of caudal fin rays are informed by both external signals from the regenerating organ and remembered identity autonomous to the local tissue [ bioRxiv, 2024, 2024.03.29.586899] | PubMed: 38585773 |
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。