Tacrolimus monohydrate

Catalog No.S5788 Batch:S578801

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Technical Data

Formula

C44H69NO12.H2O
Molecular Weight 822.04 CAS No. 109581-93-3
Solubility (25°C)* In vitro DMSO 100 mg/mL (121.64 mM)
Ethanol 100 mg/mL (121.64 mM)
Water Insoluble
In vivo (Add solvents to the product individually and in order)
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O

Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.

 5.000mg/ml (6.08mM) Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
Clear solution
5% DMSO 95% Corn oil

Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.

 2.500mg/ml (3.04mM) Taking the 1 mL working solution as an example, add 50 μL of 50 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description Tacrolimus monohydrate (Tacrolimus, FK506) is a macrolide antibiotic that primarily acts as an inhibitor of calcineurin phosphatase by binding to FK506 binding protein (FKBP). This inhibition blocks calcium-dependent processes, including interleukin-2 gene transcription, nitric oxide synthase activation, cell degranulation, and apoptosis, and also has immunosuppressive, neuroregenerative and neuroprotective properties.
Targets
calcineurin phosphatase [1]

Protocol (from reference)

References

  • https://pubmed.ncbi.nlm.nih.gov/8588225/
  • https://pubmed.ncbi.nlm.nih.gov/15198862/

Selleck's Tacrolimus monohydrate Has Been Cited by 6 Publications

Effects of Tacrolimus and Other Immune Targeting Compounds on Binge-Like Ethanol Drinking in High Drinking in the Dark Mice [ Neuroscience Insights, November 25, 2020, 2633105520975412] PubMed: 33294845
Low-dose Pimecrolimus, an FDA-approved Calcineurin Inhibitor, Sensitizes Drug-resistant Cancer Cells via Strong P-gp Inhibition [ Anticancer Research, March 2023, 1103-1112] PubMed: 36854528
Inhibition of inositol kinase B controls acute and chronic graft-versus-host disease [ Blood, January 2, 2020, 28-40] PubMed: 31697815
Validation of a dried blood spot method to measure tacrolimus concentrations in small volumes of mouse blood [ Bioanalysis, April 2022, 441-449] PubMed: 35289217
FK506-binding protein 5 regulates cell quiescence-proliferation decision in zebrafish epithelium [ FEBS Letters, 2023, 1786-1798] PubMed: 37259581
Administration of FK506 from Late Stage of Disease Prolongs Survival of Human Prion-Inoculated Mice [ Neurotherapeutics, 2020, 1850-1860] PubMed: 32483654

RETURN POLICY
Selleck Chemical’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.

SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.