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Tacrolimus (Alias: Fujimycin, FR900506, FK506)

Name: Tacrolimus
Brand: TargetMol
SKU: T2144
Price: 38 USD
Availability: InStock
Rating: 5 (10 reviews)

Catalog No. T2144 Copy Product Info

Purity: 99.94%

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Tacrolimus (FK506, Fujimycin) is a macrolide immunosuppressant that binds to FKBP12 to form a high-affinity complex (Ki = 0.2 nM), which inhibits calcineurin phosphatase activity, thereby suppressing T lymphocyte signal transduction and the transcription and release of IL-2. It exerts potent immunosuppressive effects and can be used to induce immunosuppression models.

Tacrolimus

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Catalog No. T2144

Alias Fujimycin, FR900506, FK506

Cas No. 104987-11-3

Pack Size	Price	USA Stock	Global Stock
10 mg	$38	In Stock	In Stock
25 mg	$55	In Stock	In Stock
50 mg	$68	In Stock	In Stock
100 mg	$106	In Stock	In Stock
200 mg	$150	In Stock	In Stock
500 mg	$256	-	In Stock
1 mL x 10 mM (in DMSO)	$46	In Stock	In Stock

In stock · Estimated delivery: USA Stock (1-2 days) Global Stock (5-7 days)

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For research use only—not for human use. No sales to individuals. Use as intended only.

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Purity:99.94%

Color:White

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Product Introduction

Bioactivity

Description	Tacrolimus (FK506, Fujimycin) is a macrolide immunosuppressant that binds to FKBP12 to form a high-affinity complex (Ki = 0.2 nM), which inhibits calcineurin phosphatase activity, thereby suppressing T lymphocyte signal transduction and the transcription and release of IL-2. It exerts potent immunosuppressive effects and can be used to induce immunosuppression models.
Targets&IC50	SN-38 glucuronidation (human liver microsomes):3.58 μM, Lymphocyte proliferation:0.47 nM, SN-38 glucuronidation (rat liver microsomes):10.33 μM, FKBP12:0.2 nM (Kd), Number of circulating helper-T cells:6.7 ng/mL
In vitro	FKBP12 was first isolated from the cytosol of Jurkat T cells, as an abundant, high-affinity receptor for Tacrolimus (FK506; Kd: 0.2 nM) [1]. FK506 (100?1,000 μg/l) significantly promoted the proliferation of MH3924A cells. The invasiveness of MH3924A cells was significantly enhanced following treatment with FK506 [2]. FK506 specifically inhibits cellular calcineurin at drug concentrations that inhibit interleukin 2 productions in activated T cells [3].
In vivo	The liver of rats of the normal saline (NS) group was large, with an average weight at 15.56±11.17 g, and the liver of rats of the FK506 group was oversize, with an average weight at 28.19±3.89 g. The rate of lymph node metastasis, as well as the number of pulmonary nodules, were significantly increased in the FK506 compared to the NS group [2]. Behavioral pain assessment revealed an increase in the paw and tail withdrawal threshold in tacrolimus-treated groups against hyperalgesic and allodynic stimuli as compared to the sham control group [4].
Disease Modeling Protocol	Hereditary Peripheral Demyelinating Disease Exacerbation Model Modeling Mechanism： Tacrolimus, as a calcineurin inhibitor, has the following core mechanism of action: ① It specifically binds to the immunoaffinity protein FK-binding protein 12 (FKBP12), forming a complex that inhibits calcineurin activity and blocks the NFAT signaling pathway for T cell activation, which should suppress immune inflammation. However, in hereditary peripheral demyelinating disease models (such as P0 heterozygous mice and PLP overexpression mice), its non-selective immunosuppressive effect disrupts the balance of neural tissue repair, failing to target and eliminate pro-inflammatory macrophages, and instead inhibiting the function of immune cells related to myelin repair; ② It interferes with the physiological function of glial cells (Schwann cells, astrocytes), exacerbating myelin structural disorder and axonal damage. Related Products： Tacrolimus (T2144) Modeling Method： Experimental Subject： Mice, P0 heterozygous mutant mice (P0+/-), PLP overexpression mice (PLP-OE), 6–8 weeks of age Dosage and Administration Route： ① Baseline model screening: Select naturally occurring mice; confirm demyelination phenotype via nerve conduction velocity testing (≥20% reduction in conduction velocity compared to wild-type); ② Core modelling (drug intervention): Tacrolimus, 1–5 mg/kg, dissolved in physiological saline+5% ethanol (solubiliser), intraperitoneal injection; ③ Control groups: - Model control group: Injection of equivalent volume saline+5% ethanol; - Drug toxicity control: Wild-type mice injected with equivalent Tacrolimus dose; Dosing Frequency and Duration Model： Once daily for 4–8 consecutive weeks Validation： 1. Pathological indicators: - Demyelination degree: Toluidine blue staining of sciatic nerve semi-thin sections showed that the myelin density in the Tacrolimus group decreased by ≥30%, the area of demyelinated lesions increased compared with the control group (p<0.05), and axonal arrangement was disordered; - Immune infiltration: There was no significant reduction in the infiltration of CD11b⁺ macrophages and CD3⁺ T cells in nerve tissue, and the proportion of pro-inflammatory macrophages (iNOS⁺) remained high; 2. Functional indicators: - Nerve conduction velocity: It was further slowed by ≥25% compared with before intervention, the latency of the Rotarod test was shortened by ≥40% (p<0.01), and motor function was significantly reduced; 3. Molecular indicators: - Repair-related factors: The expression of myelin basic protein (MBP) and neurotrophic factor (NGF) mRNA decreased by ≥25% compared with the control group (p<0.05), and there was no significant downregulation of inflammatory factors (TNF-α, IL-6). Precautions： References：Ip CW,et,al. Tacrolimus (FK506) causes disease aggravation in models for inherited peripheral myelinopathies. Neurobiol Dis. 2009 Feb;33(2):207-12.
Cell Research	Tumor cell proliferation was determined by the MTT. Briefly, after MH3924A cells had reached the logarithmic growth phase, a 0.2-ml cell suspension at 1×10^4 cells/ml was added into each well of a 96-well plate and cultured in DMEM with 10% FBS, 10 μg/l vascular endothelial growth factor and 0.1 g/l heparin for 24 h. When adherent growth was established, different concentrations of FK506 (10, 100 and 1,000 μg/l), AMD3100 (10, 50 and 100 μg/l) and FK506 (0 and 100 μg/l) + AMD3100 (0, 10, 50 and 100 μg/l) were added into the plates. Untreated cells cultured in medium alone were used as controls. After culturing for 48 h, 10 μl MTT (5 g/l) was added, and each well was incubated for 6 h; next, 150 μl/well dimethyl sulfoxide was added, followed by measurements of the absorbance at 570 mm on a spectrophotometer reader. Each well was measured three times, and each sample was assayed in triplicate [2].
Animal Research	Experiments were performed in 16 healthy August Copenhagen Irish rats (male, 16–20 weeks, weighing 240–300 g). The rat model of liver tumor was established as follows: First, MH3924A cells were collected and injected into the alar skin of rats. The tumors were removed from alar skin when grown to 2×1×1 mm3, and intrahepatic tumor implantation of rats was performed under aseptic conditions as described previously (25,26). Five days later, rats were randomly divided into two groups: one group was subcutaneously injected with normal saline for 14 days (NS group, n=8, 3 mg/kg/day), and the second group was subcutaneously injected with FK506 for 14 days (FK506 group, n=8, 0.3 mg/kg/day). Forty days following implantation, rats were sacrificed, and the weight of tumor, the volume of the fluid in the ascites, the incidence of lymphatic metastasis in the abdominal cavity and of abdominal wall metastasis were measured. In addition, the lungs were irrigated with 15% Indian ink, followed by counting of the number of metastatic nodules in the lung. The tumor and adjacent tissues, as well as healthy liver tissues, were harvested and preserved in 4% formalin for later use [2].
Synonyms	Fujimycin, FR900506, FK506

Chemical Properties

Molecular Weight	804.02
Formula	C₄₄H₆₉NO₁₂
Cas No.	104987-11-3
Smiles	CO[C@@H]1C[C@@H](CC[C@H]1O)\C=C(/C)[C@H]1OC(=O)[C@@H]2CCCCN2C(=O)C(=O)[C@]2(O)O[C@@H]([C@H](C[C@H]2C)OC)[C@H](C[C@@H](C)C\C(C)=C\[C@@H](CC=C)C(=O)C[C@H](O)[C@H]1C)OC
Relative Density.	1.19 g/cm3

Storage & Solubility Information

Storage

keep away from direct sunlight,store under nitrogen,store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

Ethanol: 80.4 mg/mL (100 mM), Sonication is recommended.

DMSO: 247.5 mg/mL (307.83 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 8.05 mg/mL (10.01 mM), Solution.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

Ethanol/DMSO

	1mg	5mg	10mg	50mg
1 mM	1.2438 mL	6.2188 mL	12.4375 mL	62.1875 mL
5 mM	0.2488 mL	1.2438 mL	2.4875 mL	12.4375 mL
10 mM	0.1244 mL	0.6219 mL	1.2438 mL	6.2188 mL
20 mM	0.0622 mL	0.3109 mL	0.6219 mL	3.1094 mL
50 mM	0.0249 mL	0.1244 mL	0.2488 mL	1.2438 mL
100 mM	0.0124 mL	0.0622 mL	0.1244 mL	0.6219 mL

Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density.

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc