Tacrolimus (FK506) (Synonyms: Tacrolimus)

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

Catalog No.GC16233

Tacrolimus (FK506), un antibiótico macrólido con potentes efectos inmunosupresores, fue aislado de Streptomyces tsukubaensis y ha sido utilizado previamente para prevenir el rechazo de trasplantes y para el tratamiento de trastornos autoinmunitarios en humanos.

Products are for research use only. Not for human use. We do not sell to patients.

Tacrolimus (FK506) Chemical Structure

Cas No.: 104987-11-3

Tamaño

Precio

Disponibilidad

Cantidad

10mM (in 1mL DMSO)	38,00 $	Disponible
50mg	45,00 $	Disponible
100mg	82,00 $	Disponible
200mg	130,00 $	Disponible
500mg	238,00 $	Disponible
1g	306,00 $	Disponible

Tel：(909) 407-4943 Email: sales@glpbio.com

Reseñas de cliente

Based on customer reviews.

Sample solution is provided at 25 µL, 10mM.

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

Description Protocol Chemical Properties Product Documents

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.

El tacrolimus (FK506), un antibiótico macrólido con potentes efectos inmunosupresores, fue aislado de Streptomyces tsukubaensis y ha sido utilizado previamente para prevenir el rechazo de trasplantes y para el tratamiento de trastornos autoinmunitarios en humanos^[1-3].

Tacrolimus (FK506) (0-2 µM; 24 h) reduce la síntesis de proteína de colágeno tipo I sin afectar la expresión del ARNm de colágeno en fibroblastos pulmonares humanos (HLFs)^[8]. La proliferación de células T en respuesta a la ligadura del receptor de células T es inhibida por tacrolimus(FK506)^[4]. Tacrolimus(FK506) (gradiente de concentración; 48 h) inhibió la progresión del carcinoma oral de células escamosas (OSCC) in vitro^[9].

Tacrolimus (FK506) se administró por vía intramuscular a una dosis de 0,5 y 1,0 mg/kg durante tres días antes de la lesión por quemadura. El trauma térmico en la piel causó un aumento estadísticamente significativo en la actividad de MPO y el contenido de MDA en órganos remotos. Tacrolimus (FK506) fue efectivo para reducir la peroxidación lipídica y la infiltración neutrofílica especialmente a las 24 horas después de la lesión en pulmón, hígado y riñón^[5]. Tacrolimus (FK506) tiene la capacidad de regular a la baja los niveles de radicales libres en isquemia-reperfusión severa del hígado, y también se ha demostrado que es un inhibidor efectivo de respuesta citocínica^[6]. Un estudio sobre fibrosis pulmonar en ratones sugirió que FK506 puede ser un potente agente antifibrótico ^[7]. El tratamiento con tacrolimus (FK506) inhibió la activación o redujo el número de células estrelladas hepáticas en el hígado. In vivo, la administración de tacrolimus (FK506) a una dosis de 4 mg/kg(i.p.; 4 semanas) previno completamente el desarrollo inducido por alcohol/tetracloruro carbono fibrosis hepática en ratas^[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
Sinónimos	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

Molarity Calculator
Dilution Calculator

Calculate

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.
3. All of the above co-solvents are available for purchase on the GlpBio website.

Reseñas

Review for Tacrolimus (FK506)

Average Rating: 5 ★★★★★ (Based on Reviews and 26 reference(s) in Google Scholar.)

5 Star

100%

4 Star

3 Star

2 Star

1 Star

Review for Tacrolimus (FK506)

GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.

Required fields are marked with *

Overall Rating

★

Review Title

Reseña

Apodo

Correo electrónico

You may receive emails regarding this submission. Any emails will include the ability to opt-out of future communications.

Tacrolimus (FK506) (Synonyms: Tacrolimus)

Reseñas de cliente

GlpBio Citations

Bioactive Compounds Premium Provider

GlpBio Products Cited In Reputable Papers

Product Documents

Quality Control & SDS

Protocol

Complete Stock Solution Preparation Table

Molarity Calculator

Dilution Calculator

In vivo Formulation Calculator (Clear solution)

Reseñas

Tacrolimus (FK506) (Synonyms: Tacrolimus)

Reseñas de cliente

GlpBio Citations

Bioactive Compounds Premium Provider

GlpBio Products Cited In Reputable Papers

Product Documents

Quality Control & SDS

Protocol

Complete Stock Solution Preparation Table

Molarity Calculator

Dilution Calculator

In vivo Formulation Calculator (Clear solution)

Related Products

Reseñas