Tacrolimus (FK506) is a potent immunosuppressant belonging to the macrolide lactone family. It exerts its effects by binding to FKBP12 (FK506-binding protein), forming a complex that inhibits the phosphatase activity of calcineurin, thereby preventing T-cell activation and IL-2 transcription. Tacrolimus is widely used in transplant medicine, autoimmune disease research, and neuroprotection studies.
With a purity of 99.97%, this compound is suitable for in vitro cell-based assays, biochemical studies, and in vivo animal models. It also plays a role in vascular endothelial autophagy and neuroprotection.
Key Features & Benefits
1. High-Purity Immunosuppressant for Research
- 99.97% purity ensures reliable and reproducible experimental results.
- Selectively binds FKBP12, leading to calcineurin inhibition and T-cell suppression.
- Widely used in transplantation and autoimmune disease studies.
2. Proven Mechanism in T-Cell Suppression & Inflammation Regulation
- Blocks IL-2 transcription, preventing T-cell proliferation.
- Binds immunophilins (cyclophilins & FK506-binding proteins, FKBPs), modulating immune response.
- Inhibits apoptosis and cytokine release in immune cells.
3. Versatile Research Applications (In Vitro & In Vivo Studies)
- Used in cancer immunotherapy research.
- Evaluates neuroprotective effects in ischemia-reperfusion models.
- Investigates immunosuppressive mechanisms in transplant models.
4. Ready-to-Use for Laboratory Experiments
- Provided in powder form for long-term stability (-20°C storage).
- Soluble in DMSO, ethanol, and methanol for flexible experimental use.
- Aliquot stock solutions to avoid repeated freeze-thaw cycles.
Mechanism of Action
In Vitro Studies
- Blocks nuclear translocation of cytoplasmic NF-AT (nuclear factor of activated T cells).
- Inhibits calcium-dependent T-cell activation & IL-2 production.
- Regulates immune cell apoptosis & degranulation.
Cell Line | Concentration | Incubation Time | Methodology |
---|
Jurkat T cells | 10 nM | 1 hour | Phosphatase activity assay |
In Vivo Studies
- Improves pain threshold and reduces inflammatory responses in animal models.
- Reduces oxidative stress and neuronal damage in ischemia-reperfusion injury models.
- Modulates myeloperoxidase (MPO) activity and glutathione levels in rat tissues.
Animal Model | Dosage | Administration Route |
---|
Male C57BL/6J mice | 30 mg/kg | Oral |
Chemical & Solubility Information
Property | Details |
---|
Molecular Formula | Property | Details |
---|
Molecular Formula | C₄₄H₆₉NO₁₂ | Molecular Weight | 804.02 g/mol | CAS Number | 104987-11-3 | Storage Conditions | -20°C (Powder) | Solubility | DMSO, Ethanol, Methanol | Stability in Solution | 1 month at -20°C, 1 year at -80°C | Structural Formula | Macrolide lactone with FKBP12-binding domain | C₄₄H₆₉NO₁₂ |
Molecular Weight | 804.02 g/mol |
CAS Number | 104987-11-3 |
Storage Conditions | -20°C (Powder) |
Solubility | DMSO, Ethanol, Methanol |
Stability in Solution | 1 month at -20°C, 1 year at -80°C |
Structural Formula | Macrolide lactone with FKBP12-binding domain |
Clinical & Research Applications
1. Transplantation & Autoimmune Disease Research
- Prevention of organ transplant rejection.
- Suppression of autoimmune responses in lupus, rheumatoid arthritis, and psoriasis.
2. Cancer Immunotherapy
- Investigation of calcineurin-NFAT signaling in cancer progression.
- Study of FKBP12 inhibition in tumor microenvironments.
3. Neuroprotection & Ischemia Research
- Evaluation of FK506-induced neuroprotection in stroke models.
- Potential therapeutic applications in neurodegenerative diseases (Parkinson’s, Alzheimer’s).
4. Inflammatory Disease Studies
- Modulation of cytokine expression in inflammation models.
- Assessment of Tacrolimus in chronic inflammatory diseases.
Clinical Trial Information
NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Phase |
---|
NCT05702931 | Not yet recruiting | Hyperglycemia, Renal Transplant Complication | Rigshospitalet Denmark, Aarhus University Hospital | Phase 4 |
NCT06268769 | Recruiting | Immunosuppression | Edward Geissler, Chiesi Pharmaceuticals | Phase 4 |
NCT06326775 | Active, not recruiting | Heart Transplant Patients | Nanjing First Hospital, Wuhan Union Hospital | - |
NCT06235892 | Not yet recruiting | Organ Grafts | Nantes University Hospital | Phase 3 |
Storage & Handling
- Store powder at -20°C for long-term stability.
- Prepare stock solutions in DMSO, ethanol, or methanol.
- Aliquot stock solutions to avoid repeated freeze-thaw cycles.
Ordering Information
Catalog Number | Description | Quantity |
---|
Selleckchem Tacrolimus (FK506), 99.97% | High-purity immunosuppressant for research | Various |
Selleckchem Tacrolimus (FK506), 99.97% is a high-purity immunosuppressant used in transplant medicine, autoimmune disease research, neuroprotection studies, and inflammation modulation. It functions by binding FKBP12, inhibiting calcineurin, and blocking IL-2 transcription, making it a valuable tool for immunology, cancer therapy, and neuroscientific research.
https://www.labmartgh.com/shop/product/tacrolimus-fk506-99-97-29477
-
Pack Size:
50mg
1g
500mg
10mM (1mL in DMSO)
Resources file not found.