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Tacrolimus (FK506)

Name: Tacrolimus (FK506)
Brand: Selleck Chemicals
SKU: S5003
Rating: 5 (99 reviews)

Synonyms: FR900506, Fujimycin

Catalog No.S5003 Purity:99.97%

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.

Tacrolimus (FK506) Chemical Structure

CAS No. 104987-11-3

Purity & Quality Control

Batch: Purity: 99.97%

99.97

Tacrolimus (FK506) Related Products

Related Targets	FKBP1 FKBP12	Click to Expand
Related Products	Shield-1 AP20187	Click to Expand
Related Compound Libraries	Kinase Inhibitor Library PI3K/Akt Inhibitor Library Apoptosis Compound Library Cell Cycle compound library NF-κB Signaling Compound Library	Click to Expand

Cell Data

Cell Lines	Assay Type	Incubation Time	Activity Description	PMID
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
human T-cell	Proliferation assay		In vitro inhibitory activity against human T-cell proliferation, IC50=0.5 nM	7537331
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	22410084
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
PBMCs	Function assay		Inhibitory activity against IFN-gamma production (Anti-CD3 monoclonal antibody stimulated and cultured CD4 positive cells purified from human peripheral blood mononuclear cell), IC50 = 0.00006 μM.	15369399
PBMCs	Function assay		Inhibitory activity against IL-5 production (Anti-CD3 monoclonal antibody stimulated and cultured CD4 positive cells purified from human peripheral blood mononuclear cell), IC50 = 0.00006 μM.	15369399
T-cells	Function assay		The compound was tested for its inhibitory activity against T-cell proliferation using murine splenic T-cells, IC50 = 0.0002 μM.	10450987
RBL-2H3	Function assay		Inhibition of DNP7-BSA antigen-induced TNFalpha release in rat RBL-2H3 cells, IC50 = 0.00025 μM.	16901696
Jurkat T	Immunosuppressive assay	15 to 30 mins	Immunosuppressive activity in PMA/ionomycin stimulated human Jurkat T cells assessed as suppression of IL2 production pretreated for 15 to 30 mins followed by PMA/ionomycin addition measured after 18 to 20 hrs by ELISA, IC50 = 0.36 μM.	28412204
HEK293	Function assay		TP_TRANSPORTER: inhibition of Phalloidin uptake (Phalloidin: 1 uM) in OATP-C-expressing HEK293 cells, IC50 = 3.7 μM.	14530907
Jurkat T	Antiinflammatory assay	20 mins	Anti-inflammatory activity in PMA/ionomycin stimulated human Jurkat T cells assessed as reduction in IL-2 secretion preincubated for 20 mins followed by PMA/ionomycin stimulation measured after 12 hrs by ELISA, IC50 = 5.8 μM.	28509552
Click to View More Cell Line Experimental Data

Biological Activity

Description

Targets

FKBP12 ^[1]
(T cells)

calcineurin ^[6]

In vitro
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]
Cell Research	Cell lines	Jurkat cells
	Concentrations	10 nM
	Incubation Time	1 h
	Method	Cells were cultured in the presence of 10 nM FK 506 for 1 hr and washed, and phosphatase activity was measured in lysates.
Experimental Result Images	Methods	Biomarkers	Images	PMID
	Western blot	GluA1 / pGluA1(S845) / GluA2 / GluA3 / Calcineurin p-JNK / JNK / p-ERK / ERK / Cytochrome c / cleaved caspase-3 p-S6K(S371) / S6K / p-Erα(S167) / Erα		26455952
	Immunofluorescence	FKBP52 / p23 / hsp90 FKBP51 Tom20 / JC-1 / ROS / NF-κB		20796173
	Growth inhibition assay	Cell viability		23470533

In Vivo
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]
Animal Research	Animal Models	Male C57BL/6J mice
	Dosages	30 mg/kg
	Administration	Oral

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2024-05-22)
NCT05702931	Not yet recruiting	Hyperglycemia\|Renal Transplant Complication Primary Non-Function\|Diabetes	Rigshospitalet Denmark\|Aarhus University Hospital\|Odense University Hospital	April 1 2024	Phase 4
NCT06268769	Recruiting	Immunosuppression	Edward Geissler\|Chiesi Pharmaceuticals GmbH\|University of Regensburg	March 9 2024	Phase 4
NCT06326775	Active not recruiting	Heart Transplant Patients	Nanjing First Hospital Nanjing Medical University\|Wuhan Union Hospital China\|Changhai Hospital\|Shanghai Zhongshan Hospital	March 12 2024	--
NCT06235892	Not yet recruiting	Organ Grafts	Nantes University Hospital	February 10 2024	Phase 3

References

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Chemical Information & Solubility

Molecular Weight	804.02	Formula	C₄₄H₆₉NO₁₂
CAS No.	104987-11-3	SDF	Download Tacrolimus (FK506) SDF
Smiles	CC1CC(C2C(CC(C(O2)(C(=O)C(=O)N3CCCCC3C(=O)OC(C(C(CC(=O)C(C=C(C1)C)CC=C)O)C)C(=CC4CCC(C(C4)OC)O)C)O)C)OC)OC
Storage (From the date of receipt)	3 years-20°Cpowder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years-20°Cpowder		1 month-20°Cin solvent

In vitro
Batch:

DMSO : 100 mg/mL ( (124.37 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 100 mg/mL

Water : Insoluble

Molecular Weight Calculator

In vivo Batch: Add solvents to the product individually and in order.					In vivo Formulation Calculator
	Clear solution	5% DMSO 1 corn oil	5.0mg/ml (6.22mM)	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.	In vivo Formulation Calculator
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O	5.0mg/ml (6.22mM)	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 it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of 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	2.5mg/ml (3.11mM)	Taking the 1 mL working solution as an example, add 50 μL of 50 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Clear solution	5%DMSO 1 40%PEG 300 2 5%Tween80 3 50% ddH2O	5.0mg/ml (6.22mM)	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 (6.22mM)	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.

Preparing Stock Solutions

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

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Frequently Asked Questions

Question 1:
we would like to inject it subcutaneously into rats, Can we mix the FK506 with 5% dextrose to a concentration of 5mg/ml to prepare the solution?

Answer:
You can dissolve FK506 with DMSO to prepare the stock solution, and then dilute by 5% dextrose. However, we don't have the information about the solubility in this condiation. Or you can use the vehicle we tested: 30% PEG400/0.5% Tween80/5% propylene glycol (Solubility: 30mg/ml).

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