109581-93-3 Tacrolimus monohydrate AKSci X2641
 
 
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  X2641    
Tacrolimus monohydrate
, 98% (HPLC)
 
FK-506 monohydrate
Prograf
Fujimycin monohydrate
more..




IDENTITY
CAS Number:109581-93-3
MDL Number:MFCD11045918
MF:C44H71NO13
MW:822.03
BRN:6265275
SPECIFICATIONS & PROPERTIES
Min. Purity Spec:98% (HPLC)
Physical Form (at 20°C):Solid
Melting Point:125-133°C
Long-Term Storage:Store long-term at -20°C
DOT/IATA TRANSPORT INFORMATION
UN #:UN2811
Hazard Class:6.1; Poison
Packing Group:III
A hazmat fee may apply to certain package sizes and shipment methods. Please check pricing table for an indicator of applicable hazmat fees.

BIOLOGICAL INFO
Solubility:Insoluble in water; Soluble in methanol, acetone, ethanol, ethyl acetate, acetonitrile

REVIEW

 The mechanism of action of tacrolimus in atopic dermatitis is not known. While the following have been observed, the clinical significance of these observations in atopic dermatitis is not known. It has been demonstrated that tacrolimus inhibits T-lymphocyte activation by first binding to an intracellular protein, FKBP-12. A complex of tacrolimus-FKBP-12, calcium, calmodulin, and calcineurin is then formed and the phosphatase activity of calcineurin is inhibited. This prevents the dephosphorylation and translocation of nuclear factor of activated T-cells (NF-AT), a nuclear component thought to initiate gene transcription for the formation of lymphokines. Tacrolimus also inhibits the transcription for genes which encode IL-3, IL-4, IL-5, GM-CSF, and TNF-, all of which are involved in the early stages of T-cell activation. Additionally, tacrolimus has been shown to inhibit the release of pre-formed mediators from skin mast cells and basophils, and to downregulate the expression of FceRI on Langerhans cells.

REFERENCES
[1]Kino T, Hatanaka H, Hashimoto M, Nishiyama M, Goto T, Okuhara M, Kohsaka M, Aoki H, Imanaka H: FK-506, a novel immunosuppressant isolated from a Streptomyces. I. Fermentation, isolation, and physico-chemical and biological characteristics. J Antibiot (Tokyo). 1987 Sep;40(9):1249-55.
[2] Pritchard DI: Sourcing a chemical succession for cyclosporin from parasites and human pathogens. Drug Discov Today. 2005 May 15;10(10):688-91.
[3] Liu J, Farmer JD Jr, Lane WS, Friedman J, Weissman I, Schreiber SL: Calcineurin is a common target of cyclophilin-cyclosporin A and FKBP-FK506 complexes. Cell. 1991 Aug 23;66(4):807-15.
[4] Fukatsu S, Fukudo M, Masuda S, Yano I, Katsura T, Ogura Y, Oike F, Takada Y, Inui K: Delayed effect of grapefruit juice on pharmacokinetics and pharmacodynamics of tacrolimus in a living-donor liver transplant recipient. Drug Metab Pharmacokinet. 2006 Apr;21(2):122-5.

GLOBALLY HARMONIZED SYSTEM (GHS)

Pictograms

Signal Word
Danger

Hazard Statements
H301

Precautionary Statements
P264; P270; P301+P310; P321; P330; P405; P501


Current as of October 10, 2024


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CATEGORIES

 APIs and Bioactives > Immunomodulators


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