产品说明书

Tacrolimus

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Chemical Structure| 104987-11-3 同义名 : FK506;Fujimycin;FR900506
CAS号 : 104987-11-3
货号 : A335856
分子式 : C44H69NO12
纯度 : 98%
分子量 : 804.02
MDL号 : MFCD00869853
存储条件：

粉末 Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 145 mg/mL(180.34 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：

IP 5%DMSO+2% tween 80+H2O 0.3 mg/mL clear

IP 5%DMSO+95% corn oil 5 mg/mL clear

生物活性
靶点

  • mTOR
描述 Tacrolimus (FK506), a macrocyclic lactone, forms a complex with FK506 binding protein (FKBP). It inhibits calcineurin phosphatase, thereby blocking T-lymphocyte signal transduction and IL-2 transcription, exhibiting immunosuppressive properties [1].
作用机制 FK506 selectively inhibits the enzymatic activity of the calcium/calmodulin-dependent protein phosphatase CaN
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 数据源
human T-cell Proliferation assay In vitro inhibitory activity against human T-cell proliferation, IC50=0.5 nM 7537331
human U251 cells Function assay Inhibition of SAP130 in VEGF-stimulated human U251 cells by PLAP reporter gene assay, IC50=13.8 nM 17643112
human WiDr cells Growth inhibition assay Inhibition of SAP130 mediated cell growth in human WiDr cells, IC50=10.9 nM 17643112
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.24mL

0.25mL

0.12mL

6.22mL

1.24mL

0.62mL

12.44mL

2.49mL

1.24mL
参考文献

[1]Thomson AW, et al. Mode of action of Tacrolimus (FK506): molecular and cellular mechanisms. Ther Drug Monit. 1995 Dec;17(6):584-91.

[2]Zhu H, et al. Tacrolimus promotes hepatocellular carcinoma and enhances CXCR4/SDF 1α expression in vivo. Mol Med Rep. 2014 Aug;10(2):585-92.

[3]Okada Y, et al. Tacrolimus ameliorates dextran sulfate sodium-induced colitis in mice: implication of interleukin-1β suppression. Biol Pharm Bull. 2011;34(12):1823-7.