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Product Description
Tacrolimus, FK-506 or Fujimycin is an immunosuppressive drug that is mainly used after allogeneic organ transplant to reduce the activity of the patient's immune system and so lower the risk of organ rejection.
It is also used in a topical preparation in the treatment of atopic dermititis (eczema), severe refractory uveitis after bone marrow transplants, and the skin condition vitiligo.
br> br>Tacrolimus is chemically known as a macrolide. In T-cells, activation of the T-cell receptor normally increases intracellular calcium, which acts via calmodulin to activate calcineurin. Calcineurin then dephosphorylates the transcription factor NF-AT (nuclear factor of activated T-cells), which moves to the nucleus of the T-cell and increases the activity of genes coding for IL-2 and related cytokines. Tacrolimus prevents the dephosphorylation of NF-AT.
In detail, Tacrolimus reduces peptidyl-prolyl isomerase activity by binding to the immunophilin FKBP12 (FK506 binding protein) creating a new complex. This FKBP12-FK506 complex interacts with and inhibits calcineurin thus inhibiting both T-lymphotye signal transduction and IL-2 transcription. Although this activity is similar to cyclosporine, studies have shown that the incidence of acute rejection is reduced by tacrolimus use over cyclosporine.Although short-term immunosuppression concerning patient and graft survival is found to be similar between the two drugs, tacrolimus results in a more favorable lipid profile, and this may have important long-term implications given the prognostic influence of rejection on graft survival.
Attached are a few published references from researchers who have used our FK-506 product. We respectfully thank them for their trust in our product. Inquire for a full reference list.
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1. Nobuko Hamasaki-Katagiriand James B. Ames. “Neuronal Calcium Sensor-1(Ncs1p) Is Up-regulated by Calcineurin to Promote Ca2+ Tolerance in Fission Yeast*” J BIOL. CHEM. 285: 4405–4414,(2010).
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2. Frederick,R.L et al.” Yeast Miro GTPase, Gem1p, regulates mitochondrial morphology via a novel pathway”. J Cell Bio. 167: 87-98, (2004).
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3. Joel Karwatsky et al, ‘Cholesterol efflux to apoA-I in ABCA1-expressing cells isregulated by Ca2+-dependent calcineurin signaling.” J Lipid Res.51: 1144-1156.(2010).
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Seek researchers utilizing our FK-506 product?- br> br>
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http://dev.biologists.org/content/133/16/3107.full.pdf+html
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http://mcb.asm.org/content/30/10/2401.full.pdf+html
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http://dev.biologists.org/content/133/16/3107.full.pdf+html
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http://www.jlr.org/content/51/5/1144.full.pdf+html
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http://www.jbc.org/content/285/7/4405.full.pdf+html
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http://www.jimmunol.org/content/174/5/2720.full.pdf+html
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http://www.jleukbio.org/content/86/2/337.full.pdf+html
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http://www.jneurosci.org/content/27/48/13161.full.pdf+html
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http://ajpcell.physiology.org/content/287/4/C971.full.pdf+html
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http://www.jneurosci.org/content/29/48/15331.full.pdf+html
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http://www.jbc.org/content/280/45/37526.full.pdf+html
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http://www.jleukbio.org/content/86/2/205.full.pdf+html
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http://www.jneurosci.org/content/27/21/5683.full.pdf+html
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http://jcb.rupress.org/content/167/1/87.full.pdf+html
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http://dev.biologists.org/content/133/16/3107.full.pdf+html
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http://mcb.asm.org/content/27/2/633.full.pdf+html
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http://jeb.biologists.org/content/211/7/1102.full.pdf+html
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Additional Information
MSDS Documentation:COA Documentation: |
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| Product Number | F-1030 |
| CAS # | CAS [104987-11-3] |
| Chemical Formula | C44H69NO12 |
| Alternative Name | Tacrolimus, FR-900506, Prograf, Protopic |
| Appearance | Off-White Solid |
| Melting Point | MP: 119-121°C* |
| Merck Index | Merck Index: 13.9117.2001 |
| Molecular Weight | M.W. 804.0 |
| Preparation | Also reported to provide clear solution at >10mg/ml CH2CI2 |
| Purity | Purity: ≥99% |
| Solubility | Soluble in DMSO, MeOH, also ETOAC. |
| Storage Temp | -20°C |
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