Tacrolimus (FK506), 99.97%

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Specifications:
Application Cell culture, HPLC
Storage Temperature -20°C
Product Type Proteins & Peptides Forms Powder
Product Brand Selleckchem
Product Grade Analytical grade Formula C₄₄H₆₉NO₁₂

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 LineConcentrationIncubation TimeMethodology
Jurkat T cells10 nM1 hourPhosphatase 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 ModelDosageAdministration Route
Male C57BL/6J mice30 mg/kgOral

Chemical & Solubility Information

PropertyDetails
Molecular Formula
PropertyDetails
Molecular FormulaC₄₄H₆₉NO₁₂
Molecular Weight804.02 g/mol
CAS Number104987-11-3
Storage Conditions-20°C (Powder)
SolubilityDMSO, Ethanol, Methanol
Stability in Solution1 month at -20°C, 1 year at -80°C
Structural FormulaMacrolide lactone with FKBP12-binding domain
C₄₄H₆₉NO₁₂
Molecular Weight804.02 g/mol
CAS Number104987-11-3
Storage Conditions-20°C (Powder)
SolubilityDMSO, Ethanol, Methanol
Stability in Solution1 month at -20°C, 1 year at -80°C
Structural FormulaMacrolide 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 NumberRecruitmentConditionsSponsor/CollaboratorsPhase
NCT05702931Not yet recruitingHyperglycemia, Renal Transplant ComplicationRigshospitalet Denmark, Aarhus University HospitalPhase 4
NCT06268769RecruitingImmunosuppressionEdward Geissler, Chiesi PharmaceuticalsPhase 4
NCT06326775Active, not recruitingHeart Transplant PatientsNanjing First Hospital, Wuhan Union Hospital-
NCT06235892Not yet recruitingOrgan GraftsNantes University HospitalPhase 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 NumberDescriptionQuantity
Selleckchem Tacrolimus (FK506), 99.97%High-purity immunosuppressant for researchVarious

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.

  • Pack Size:   50mg 1g 500mg 10mM (1mL in DMSO)
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