Tacrolimus (FK506)

製品コードS5003 バッチS500316

印刷

化学情報

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

100 mg/mL (124.37 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）

Clear solution	5%DMSO 1 40%PEG 300 2 5%Tween80 3 50% ddH2O	5.0mg/ml	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/mL clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify; add 50 μL of Tween-80 to the above system, mix evenly to clarify; Then continue to add 500 μL ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5%DMSO 1 95% Corn oil	5.0mg/ml	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	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]

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	Cells were cultured in the presence of 10 nM FK 506 for 1 hr and washed, and 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

+ 展开

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：

T cell receptor signaling strength establishes the chemotactic properties of effector CD8+ T cells that control tissue-residency [ Nat Commun, 2023, 14(1):3928]	PubMed: 37402742
FKBP12 is a major regulator of ALK2 activity in multiple myeloma cells [ Cell Commun Signal, 2023, 21(1):25]	PubMed: 36717825
Calcineurin regulates aldosterone production via dephosphorylation of NFATC4 [ JCI Insight, 2023, 8(14)e157027]	PubMed: 37310791
Locally controlled release of immunosuppressive promotes survival of transplanted adult spinal cord tissue [ Regen Biomater, 2023, 10:rbac097]	PubMed: 36683735
Calcineurin-mediated dephosphorylation enhances the stability and transactivation of c-Myc [ Sci Rep, 2023, 13(1):13116]	PubMed: 37573463
FK506-binding protein 5 regulates cell quiescence-proliferation decision in zebrafish epithelium [ FEBS Lett, 2023, 10.1007/s10565-023-09816-7]	PubMed: 37259581
Tacrolimus Maintains the Balance of Neutrophil Extracellular Traps by Inducing DNA Methylation of Neutrophils to Reduce Immune Rejection [ Life (Basel), 2023, 13(12)2253]	PubMed: 38137854
Antagonistic effect of cyclin-dependent kinases and a calcium-dependent phosphatase on polyglutamine-expanded androgen receptor toxic gain of function [ Sci Adv, 2023, 9(1):eade1694]	PubMed: 36608116
Immunosuppression with Cyclosporine versus Tacrolimus shows distinctive nephrotoxicity profiles within renal compartments [ bioRxiv, 2023, 10.1101/2023.04.05.535688 ]	PubMed: none
The role of IL-18 and IL-1 receptor signaling in T cell development and T cell exhaustion in a murine pancreatic cancer model [ Philipps-Universität Marburg, 2023, 10.17192/z2023.0576]	PubMed: none

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。