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Type
HazMat fee for 500 gram (Estimated)
Excepted Quantity
USD 0.00
Limited Quantity
USD 15-60
Inaccessible (Haz class 6.1), Domestic
USD 80+
Inaccessible (Haz class 6.1), International
USD 150+
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Accessible (Haz class 3, 4, 5 or 8), International
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].
体内研究
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].
体外研究
Tacrolimus (FK506) inhibits calcium-dependent processes, including IL-2 gene transcription, NO synthase activation, cell degranulation, and apoptosis. It also enhances glucocorticoid and progesterone actions by binding to FKBPs within the hormone receptor complex, preventing degradation. Additionally, Tacrolimus may upregulate TGFβ-1 gene expression similar to CsA. T cell proliferation in response to T cell receptor ligation is inhibited by Tacrolimus [1].
Tacrolimus (10 μg/L) has no significant effect on MH3924A cell proliferation (P=0.135). However, higher concentrations (100-1,000 μg/L) significantly enhance cell proliferation (P<0.01). Treatment with AMD3100 at any concentration (10, 50, or 100 μg/L) does not visibly affect MH3924A cell proliferation (P>0.05). However, combining different concentrations of AMD3100 with 100 μg/L Tacrolimus increases in vitro MH3924A cell proliferation (P<0.01) [3].
作用机制
FK506 selectively inhibits the enzymatic activity of the calcium/calmodulin-dependent protein phosphatase CaN
Tacrolimus/他克莫司 细胞实验
Cell Line
Concentration
Treated Time
Description
References
Primary mouse cortical neurons
0.1 µM and 1 µM
72 hours
To evaluate the neuroprotective effect of NFAT inhibitors against neuron death induced by Aβ-stimulated microglial conditioned media. Results showed that conditioned media from FK506-treated microglia attenuated Aβ-stimulated neuronal toxicity.
J Neuroinflammation. 2015 Mar 4;12:42.
HEK293 cells
25 ng/mL
16 h
To evaluate the effect of Tacrolimus on COVID-19 mRNA vaccine-induced Spike protein expression, results showed that Tacrolimus did not significantly affect Spike protein expression.
Front Immunol. 2022 Oct 26;13:1020165.
Mouse Aortic Endothelial Cells
1 µm
15 min
To investigate the effect of tacrolimus on intracellular calcium levels, the results showed that tacrolimus caused intracellular calcium leakage and significantly reduced acetylcholine-induced calcium release.
Kidney Int. 2009 Apr;75(7):719-26.
Tacrolimus/他克莫司 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
ICR mice
Tacrolimus-induced chronic nephrotoxicity model
Subcutaneous injection
1 mg/kg/day
Once daily for 28 days
To investigate the relationship between tacrolimus-induced chronic nephrotoxicity and NAD+ metabolism, results showed significantly decreased NAD+ levels and increased degradation products such as nicotinamide N-oxide
Antioxidants (Basel). 2025 Jan 7;14(1):62
Balb/c mice
Healthy mice
Oral
12.5 mg/kg
Once daily for 7 days
To evaluate the effect of Tacrolimus in combination with Sirolimus and Prednisone on COVID-19 mRNA vaccine-induced IgM and IgG antibody responses, results showed that TSP pretreatment significantly attenuated IgM and IgG antibody responses.
Front Immunol. 2022 Oct 26;13:1020165.
SD rats
SD rats
Oral
0.3 mg/kg
Once daily for 14 days
To evaluate whether chimeric renal organoid transplantation can reduce xenogeneic immune rejection under mild immunosuppression
Front Immunol. 2022 Feb 15;13:848433
Mice
Immunosuppression model
Intraperitoneal injection
1 mg/kg
Once daily, continued for the duration of the study
To evaluate the protective efficacy of Tacrolimus in an immunosuppression model against pulmonary aspergillosis, results showed significantly reduced mortality and lung fungal burden in AF.KEX1-vaccinated mice
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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