Tacrolimus is a potent immunosuppressive drug often administered to transplant recipient patients and exhibits a variety of adverse cardiovascular effects. Its mechanism of action involves the formation of a high affinity complex (Ki = 0.2 nM) with FK-506 binding protein 12 (FKBP12).
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HazMat fee for 500 gram (Estimated)
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Limited Quantity
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Inaccessible (Haz class 6.1), Domestic
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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].
Tacrolimus/他克莫司 细胞研究
细胞系
浓度
检测类型
检测时间
活性说明
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
rat RBL2H3 cells
Function assay
16 h
Inhibition of TNF-alpha production in rat RBL2H3 cells after 16 hrs by ELISA, IC50=0.25 nM
23791076
Tacrolimus/他克莫司 动物研究
Animal study
The therapeutic efficacy of Tacrolimus in colitis progression and perpetuation is examined by administering it to DSS-treated mice from Days 10 to 16 or 23. Compared to normal mice, DSS-treated control animals at Days 17 and 24 exhibit significantly shortened colon length and higher colon weight. Additionally, colon weight per unit length is over double that of normal mice. Both 7 and 14-day Tacrolimus treatments significantly suppress increases in colon weight per unit length in DSS-treated animals compared to controls. However, Tacrolimus does not restore colon shortening. Moreover, the inhibitory effect of Tacrolimus on colon weight per unit length increase is more pronounced with 14-day treatment compared to 7-day treatment, as indicated by inhibitory percentages (59% vs. 28%) [4].
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
rat RBL2H3 cells
Function assay
16 h
Inhibition of TNF-alpha production in rat RBL2H3 cells after 16 hrs by ELISA, IC50=0.25 nM
23791076
rat RBL2H3 cells
Function assay
15 mins
Antiinflammatory activity in rat RBL2H3 cells assessed as inhibition of DNP-BSA-induced TNF-alpha production preincubated for 15 mins prior DNP-BSA challenge measured after 30 mins by ELISA, IC50=0.25 nM
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