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Tacrolimus (FK506)

Tacrolimus (FK506)

Catalog No.

B2143

Macrolide calcineurin inhibitor,immunosuppressant

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Grouped product items
Size	Price	Stock
10mM (in 1mL DMSO)	$55.00	In stock
50mg	$65.00	In stock
100mg	$120.00	In stock
200mg	$180.00	In stock
500mg	$310.00	In stock
1g	$480.00	In stock

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Background
Product Citation
Chemical Properties
Protocol
Biological Activity
Quality Control

Background

Tacrolimus (FK506) is a potent and selective inhibitor of T-lymphocyte and the macrolide immunosuppressant [1].

In vitro, Tacrolimus (FK506) has been reported to inhibit the interleukin 2(IL-2) production and the response of mixed lymphocyte culture. In addition, Tacrolimus (FK506) added to the cell cultures has been revealed to inhibit murine or human mixed lymphocyte reactivity and the generation of cytotoxic T cells. Furermor, Tacrolimus (FK506) has also been reported to dose-dependently suppress the production of various cytokines including IL-2, IL-3, IL-4, and γ-interferon, in response to different stimulis. Besides, Tacrolimus has shown its efficacy in the prevention of allograft rejection in animal transplant models. Tacrolimus has been found to be significantly efficient in experimental hepatic allografts, and has hepatotrophic properties [1].

References:
[1] Wallemacq PE1, Reding R. FK506 (tacrolimus), a novel immunosuppressant in organ transplantation: clinical, biomedical, and analytical aspects. Clin Chem. 1993 Nov; 39(11 Pt 1):2219-28.

Product Citation

Chemical Properties

Physical Appearance	A solid
Storage	Store at -20°C
M.Wt	804.02
Cas No.	104987-11-3
Formula	C₄₄H₆₉NO₁₂
Solubility	≥26.6 mg/mL in DMSO; insoluble in H2O; ≥84.5 mg/mL in EtOH
SDF	Download SDF
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
Shipping Condition	Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice.
General tips	We do not recommend long-term storage for the solution, please use it up soon.

Protocol

Cell experiment:
Cell lines	Liver slices, human lung fibroblasts
Preparation method	The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.
Reacting condition	2 μM and 4 μM for 3 days
Applications	FK506 reduced type I collagen synthesis in liver slices cultured in vitro [1]. Moreover, FK506 (2 μM) decreased the type I collagen protein synthesis without affecting expression of collagen mRNAs [2].
Animal experiment:
Animal models	Rats model
Dosage form	4 mg/kg; i.p. injections, daily dose for 4 weeks; or 1, 2 and 3 mg/kg, p.o. for 10 consecutive days
Applications	FK506 (4 mg/kg) prevented early stages of ethanol induced hepatic fibrosis by targeting LARP6 dependent mechanism of collagen synthesis in rats [1]. Moreover, FK506 (2 and 3 mg/kg) treatment resulted in attenuation of arterial ischemic reperfusion (I/R) induced axonal degeneration and histopathological alterations in rats [2].
Other notes	Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.
References: 1Manojlovic, Z., Blackmon, J. and Stefanovic, B. (2013) Tacrolimus (FK506) prevents early stages of ethanol induced hepatic fibrosis by targeting LARP6 dependent mechanism of collagen synthesis. PLoS One. 8, e65897 2Muthuraman, A. and Sood, S. (2010) Pharmacological evaluation of tacrolimus (FK-506) on ischemia reperfusion induced vasculatic neuropathic pain in rats. J Brachial Plex Peripher Nerve Inj. 5, 13