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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.
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 part of 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.
Calcium-dependent phosphorylation regulates neuronal stability and plasticity in a highly precise pacemaker nucleus, Andrew A. George, et al., J Neurophysiol, Jul 2011; 106: 319 - 331.
CELLULAR IMMUNOLOGY AND IMMUNE REGULATION: CpG Protects Human Monocytic Cells against HIV-Vpr–Induced Apoptosis by Cellular Inhibitor of Apoptosis-2 through the Calcium-Activated JNK Pathway in a TLR9-Independent Manner, Mansi Saxena, et al., J. Immunol., Dec 2011; 187: 5865 - 5878.
Upregulation of D2-class signaling in dopamine-denervated striatum is in part mediated by D3 receptors acting on CaV2.1 channels via PIP2 depletion, G. Aleph Prieto, et al., J Neurophysiol, May 2011; 105: 2260 - 2274.
Drp1 dephosphorylation in ATP depletion-induced mitochondrial injury and tubular cell apoptosis, Sung-Gyu Cho, et al., J Physiol Renal Physiol, Jul 2010; 299: F199 - F206.
RESEARCH ARTICLES: Cholesterol efflux to apoA-I in ABCA1-expressing cells is regulated by Ca2+-dependent calcineurin signaling, Joel Karwatsky, et al., J. Lipid Res., May 2010; 51: 1144 - 1156.
SIGNAL TRANSDUCTION: Neuronal Calcium Sensor-1 (Ncs1p) Is Up-regulated by Calcineurin to Promote Ca2+ Tolerance in Fission Yeast, Nobuko Hamasaki-Katagiri and James B. Ames, J. Biol. Chem., Feb 2010; 285: 4405 - 4414.
Phospholipase C Activation Drives Increased Production of Autotaxin in Endothelial Cells and Lysophosphatidic Acid-Dependent Regression, Eunok Im, et al., Mol. Cell. Biol., May 2010; 30: 2401 - 2410.
DEVELOPMENT/PLASTICITY/REPAIR: Nuclear Factor of Activated T-Cells Isoform c4 (NFATc4/NFAT3) as a Mediator of Antiapoptotic Transcription in NMDA Receptor-Stimulated Cortical Neurons, Aruna Vashishta, et al., J. Neurosci., Dec 2009; 29: 15331 - 15340.
RECEPTORS, SIGNAL TRANSDUCTION, & GENES: Zinc transporter ZIP8 (SLC39A8) and zinc influence IFN- expression in activated human T cells, Tolunay B. Aydemir, et al., J. Leukoc. Biol., Aug 2009; 86: 337 - 348.
NEUROBIOLOGY OF DISEASE: The Down Syndrome Critical Region Protein RCAN1 Regulates Long-Term Potentiation and Memory via Inhibition of Phosphatase Signaling, Charles A. Hoeffer,et al., J. Neurosci., Nov 2007; 27: 13161 - 13172.
CELLULAR/MOLECULAR: Cholinergic Axons Modulate GABAergic Signaling among Hippocampal Interneurons via Postsynaptic 7 Nicotinic Receptors, Nicolas Wanaverbecq, et al., J. Neurosci., May 2007; 27: 5683 - 5693.
CELLULAR IMMUNOLOGY AND IMMUNE REGULATION: IL-10 Regulation by HIV-Tat in Primary Human Monocytic Cells: Involvement of Calmodulin/Calmodulin-Dependent Protein Kinase-Activated p38 MAPK and Sp-1 and CREB-1 Transcription Factors, Katrina Gee, et al., J. Immunol., Jan 2007; 178: 798 - 807.
MEMBRANE TRANSPORT, STRUCTURE, FUNCTION, AND BIOGENESIS: Protein Kinase C-dependent Enhancement of Activity of Rat Brain NCKX2 Heterologously Expressed in HEK293 Cells, Ju-Young Lee, et al., J. Biol. Chem., Dec 2006; 281: 39205 - 39216.
MECHANISMS OF SIGNAL TRANSDUCTION: Distinct Role of Calmodulin and Calmodulin-dependent Protein Kinase-II in Lipopolysaccharide and Tumor Necrosis Factor--mediated Suppression of Apoptosis and Antiapoptotic c-IAP2 Gene Expression in Human Monocytic Cells Sasmita Mishra, Jyoti P. Mishra, et al., J. Biol. Chem., Nov 2005; 280: 37536 - 37546.
Additional Information
| 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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![FK-506 | Tacrolimus | CAS[104987-11-3]| Immunosuppressant | A.G. Scientific | Structure image](http://www.agscientific.com/media/catalog/product/cache/1/thumbnail/56x/5e06319eda06f020e43594a9c230972d/f/i/file_4_19.png "FK-506 | Tacrolimus | CAS[104987-11-3]| Immunosuppressant | A.G. Scientific | Structure image")
![FK-506 | Tacrolimus | CAS[104987-11-3]| Immunosuppressant | A.G. Scientific | Bound to immunosuppressants](http://www.agscientific.com/media/catalog/product/cache/1/thumbnail/56x/5e06319eda06f020e43594a9c230972d/f/i/file_6_5.jpg "FK-506 | Tacrolimus | CAS[104987-11-3]| Immunosuppressant | A.G. Scientific | Bound to immunosuppressants")
![FK-506 | Tacrolimus | CAS[104987-11-3]| Immunosuppressant | A.G. Scientific | Binding FK-506](http://www.agscientific.com/media/catalog/product/cache/1/thumbnail/56x/5e06319eda06f020e43594a9c230972d/f/i/file_5_17.jpg "FK-506 | Tacrolimus | CAS[104987-11-3]| Immunosuppressant | A.G. Scientific | Binding FK-506")
![FK-506 | Tacrolimus | CAS[104987-11-3]| Immunosuppressant | A.G. Scientific | Binding to other proteins](http://www.agscientific.com/media/catalog/product/cache/1/thumbnail/56x/5e06319eda06f020e43594a9c230972d/f/i/file_6_4.gif "FK-506 | Tacrolimus | CAS[104987-11-3]| Immunosuppressant | A.G. Scientific | Binding to other proteins")
![FK-506 | Tacrolimus | CAS[104987-11-3]| Immunosuppressant | A.G. Scientific | 3-D Image](http://www.agscientific.com/media/catalog/product/cache/1/thumbnail/56x/5e06319eda06f020e43594a9c230972d/f/i/file_5_15.gif "FK-506 | Tacrolimus | CAS[104987-11-3]| Immunosuppressant | A.G. Scientific | 3-D Image")
