Name: Tacrolimus (FK506)
Brand: GlpBio
SKU: GC16233
Availability: InStock
Rating: 5 (26 reviews)

GlpBio Products Cited In Reputable Papers

Nature
610.7931 (2022): 366-372

Nature
618, 1017–1023 (2023)

Cell
183.7 (2020): 1867-1883

Cell Research
31, 1291–1307 (2021)

Cell Research
33, 273–287 (2023)

Cell Research
33, 546–561 (2023)

Molecular Cancer
21.1 (2022): 1-17

Molecular Cancer
21.1 (2022): 1-18

Cancer Cell
39 (2021): 1-16

Cell Host Microbe
30.8 (2022): 1124-1138

Cell Host Microbe
31.5 (2023): 766-780

Cell Host Microbe
31.3 (2023): 418-43

Cell Metabolism
34.2 (2022): 240-255

Ann Rheum Dis
82(4): 533-545 (2023)

Cell Mol Immunol
20, 264–276 (2023)

Adv Funct Mater
33.35 (2023): 2214998

Product Documents

Quality Control & SDS

View current batch:

Purity: >99.90%

Protocol

Cell experiment [1]:
Cell lines	Human lung fibroblasts (HLFs)
Preparation Method	Cells were incubated with the indicated concentrations of FK506 for 24 h. The cells were then washed 3 times with PBS and incubated for 3 h in serum free medium to accumulate secreted collagen.
Reaction Conditions	0-2 µM Tacrolimus (FK506);24 h
Applications	Tacrolimus (FK506) reduces synthesis of type I collagen protein.
Animal experiment [2]:
Animal models	Male inbred alki Wistar rats weighing 150-200 g
Preparation Method	At the start of the study, drinking water was replaced by 5% ethanol as the only source of liquid and the rats were allowed to drink at will. Carbon tetrachloride (CCl4) was administered intraperitoneally (i.p.) at 0.5 µl/g of CCl4 in mineral oil twice a week for 4 weeks. Tacrolimus (FK506) was dissolved in 200 µL of Cremaphor and injected at daily dose of 4 mg/kg for 4 weeks (28 days). Control animals received by i.p. injections the Cremaphor vehicle. The groups were as follows: group 1:5% ethanol liquid+CCl4 injections; group 2:5% ethanol liquid+CCl4 injections+FK506 treatment; group 3: FK506 treatment only; group 4: vehicle only.
Dosage form	4 mg/kg;4 weeks (28 days);i.p.
Applications	Tacrolimus (FK506) treatment inhibited activation of hepatic stellate cells (HSC) or reduced their number in the liver. In vivo, administration of FK506 at a dose of 4 mg/kg completely prevented development of alcohol/carbon tetrachloride induced liver fibrosis in rats.
References: [1].Manojlovic Z, Blackmon J, et,al. Tacrolimus (FK506) prevents early stages of ethanol induced hepatic fibrosis by targeting LARP6 dependent mechanism of collagen synthesis. PLoS One. 2013 Jun 3;8(6):e65897. doi: 10.1371/journal.pone.0065897. PMID: 23755290; PMCID: PMC3670911.

Tacrolimus (FK506), a macrolide antibiotic with potent immunosuppressive effects was isolated from Streptomyces tsukubaensis and has been previously used to prevent allograft and for treatment of autoimmune disorders in humans^[1-3].

Tacrolimus(FK506) (0-2 µM;24 h)reduces synthesis of type I collagen protein without affecting expression of collagen mRNAs in Human lung fibroblasts (HLFs)^[8]. T cell proliferation in response to ligation of the T cell receptor is inhibited by tacrolimus(FK506) ^[4]. Ttacrolimus(FK506) (concentration gradient;48 h)inhibited oral squamous cell carcinoma (OSCC) progression in vitro ^[9].

Tacrolimus (FK506) was given intramuscularly at the dose of 0.5 and 1.0 mg/kg for three days before burn injury. Thermal trauma to the skin caused a statistically significant increase in MPO activity and MDA content in remote organs. Tacrolimus (FK506) was effective in reducing lipid peroxidation and neutrophil infiltration especially at 24 h postinjury in lung, liver and kidney^[5]. Tacrolimus (FK506) has the ability to down-regulate free radical levels in severe ischemia-reperfusion liver, and tachlimus has also been shown to be an effective inhibitor of cytokine response^[6]. A study on pulmonary fibrosis in mice suggested that FK506 can be a potent antifibrotic agent ^[7]. Tacrolimus (FK506) treatment inhibited activation of HSCs or reduced their number in the liver. In vivo, administration of Tacrolimus (FK506) at a dose of 4 mg/kg(i.p.; 4 weeks) completely prevented development of alcohol/carbon tetrachloride induced liver fibrosis in rats^[8].

References:
[1]. Wiederrecht G, Lam E, et,al. The mechanism of action of FK-506 and cyclosporin A. Ann N Y Acad Sci. 1993 Nov 30;696:9-19. doi: 10.1111/j.1749-6632.1993.tb17137.x. PMID: 7509138.
[2]. Kino T, Hatanaka H, et,al. FK-506, a novel immunosuppressant isolated from a Streptomyces. II. Immunosuppressive effect of FK-506 in vitro. J Antibiot (Tokyo). 1987 Sep;40(9):1256-65. doi: 10.7164/antibiotics.40.1256. PMID: 2445722.
[3]. Kondo H, Abe T, et,al. Efficacy and safety of tacrolimus (FK506) in treatment of rheumatoid arthritis: a randomized, double blind, placebo controlled dose-finding study. J Rheumatol. 2004 Feb;31(2):243-51. PMID: 14760792.
[4]. Thomson AW, Bonham CA, et,al.Mode of action of tacrolimus (FK506): molecular and cellular mechanisms. Ther Drug Monit. 1995 Dec;17(6):584-91. doi: 10.1097/00007691-199512000-00007. PMID: 8588225.
[5]. Cetinkale O, Konukoğlu D, et,al. Modulating the functions of neutrophils and lipid peroxidation by FK506 in a rat model of thermal injury. Burns. 1999 Mar;25(2):105-12. doi: 10.1016/s0305-4179(98)00147-8. PMID: 10208383.
[6]. Garcia-Criado FJ, Palma-Vargas JM, et,al.Tacrolimus (FK506) down-regulates free radical tissue levels, serum cytokines, and neutrophil infiltration after severe liver ischemia. Transplantation. 1997 Aug 27;64(4):594-8. doi: 10.1097/00007890-199708270-00008. PMID: 9293871.
[7]. Nagano J, Iyonaga K, et,al.Use of tacrolimus, a potent antifibrotic agent, in bleomycin-induced lung fibrosis. Eur Respir J. 2006 Mar;27(3):460-9. doi: 10.1183/09031936.06.00070705. PMID: 16507844.
[8]. Manojlovic Z, Blackmon J, et,al.Tacrolimus (FK506) prevents early stages of ethanol induced hepatic fibrosis by targeting LARP6 dependent mechanism of collagen synthesis. PLoS One. 2013 Jun 3;8(6):e65897. doi: 10.1371/journal.pone.0065897. PMID: 23755290; PMCID: PMC3670911.
[9]: Li Y, Wang Y, et,al. Tacrolimus inhibits oral carcinogenesis through cell cycle control. Biomed Pharmacother. 2021 Jul;139:111545. doi: 10.1016/j.biopha.2021.111545. Epub 2021 Apr 16. PMID: 33873145.

Cas No.	104987-11-3	SDF
Synonyms	Tacrolimus
Canonical SMILES	CO[C@@H]1C[C@H](/C=C(C)/[C@@H](OC([C@]2([H])CCCCN2C(C([C@]3(O)O[C@H]([C@@H](OC)C[C@H](C/C(C)=C/4)C)[C@@H](OC)C[C@H]3C)=O)=O)=O)[C@H](C)[C@H](CC([C@@H]4CC=C)=O)O)CC[C@H]1O
Formula	C₄₄H₆₉NO₁₂	M.Wt	804.02
Solubility	≥ 26.6mg/mL in DMSO, ≥ 84.5 mg/mL in EtOH	Storage	4°C, protect from light
General tips	Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition	Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

Prepare stock solution
		1 mg	5 mg	10 mg
	1 mM	1.2438 mL	6.2188 mL	12.4375 mL
	5 mM	0.2488 mL	1.2438 mL	2.4875 mL
	10 mM	0.1244 mL	0.6219 mL	1.2438 mL

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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. )

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Tacrolimus (FK506) (Synonyms: Tacrolimus)

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