Tacrolimus Monohydrate Antibiotic Immunosuppressant

English name: Tacrolimus Monohydrate
CAS number:109581-93-3
Molecular formula: C44H71NO13
Molecular weight:822.05
EINECS No:617-559-7
Related categories:
Tacrolimus impurities; medical raw material; fermentation; pharmaceutical raw material; chemical connection; drug substance; antibiotics; medical raw material; chemical reagents; chemical raw material; raw material; Signalling; fine chemical raw material.
The Mol file: 109581-93-3.mol

Structural formula:

Ttacrolimus monohydrate properties
Melting point: 127-129
Specific rotation: D23-84.4 (c = 1.02 in chloroform)
Storage conditions: -20 C
Solubility: DMSO: soluble, 20 mg/mL
Form: powder
Color: White to almost white
Merck:14,9025
InChIKey:NWJQLQGQZSIBAF-MLAUYUEBSA-N
 

 Bioactivity

Tacrolimus monohydrate (FK506 monohydrate) is a macrolide compound. Tacrolimus monohydrate binds to the FK506 binding protein (FKBP) to form a complex and inhibits calcineurin (calcineurin phosphatase), thereby inhibiting T lymphocyte signaling and IL-2 transcription. With strong immunosuppressive properties.

 Target spot

PP2B (calcineurin phosphatase)

Autophagy inducer

 In vitro study

Tacrolimus monohydrate (FK506 monohydrate; Fujimycin monohydrate; FR900506 monohydrate inhibits squamous cell dependent events such as IL-2 gene transcription, nitric oxide synthase activation, cell degranulation, and apoptosis. Tacrolimus has the potential to act as a glucocorticoid and progesterone on FKBP contained in hormone receptor complexes, preventing its degradation. This reagent may enhance the expression of TGF-1 gene demonstrated by CsA in fashion homologs. TacrChemicalbookolimus inhibits T cell proliferation and T cell receptor response. Low concentration tacrolimus (FK506, 10 μ g/L) treatment had no significant effect on the proliferation of MH3924A cells (P=0.135). Under treatment with high concentrations of tacrolimus (100-1000 μ g/L), the proliferation of MH3924AC was significantly enhanced (P<0.01). Treatment with AMD3100 concentrations (10, 50, or 100 μ g/L) had no significant effect on the proliferation of MH3924 cells (P>0.05). However, when different concentrations of AMD3100 were combined with 100 μ g/L acrolimus, the in vitro proliferation of MH3924ACell increased (P<0.01).

 In vivo research

The therapeutic effect of tacrolimus was studied for the progression and persistence of colitis by combining tacrolimus with sodium dextran (DSS) treatment in mice from day 10 to day 16 or day 23. On the 17th and 24th days, the length of the colon significantly shortened and the weight of the colon significantly increased. The control animals treated with DSS were compared to normal animals. In addition, the colon weight per unit length in the control group was more than twice that of the chemical control group. Although treatment with tacrolimus for 7 and 14 days significantly inhibited the increase in colon weight per unit length in DSS treated animals compared to the control group, this treatment did not truly restore colon shortening. In addition, the inhibitory effect of tacrolimus on the increase of colon weight per unit length was more pronounced in the 14 day and 7-day treatments, as shown by the inhibition percentage (59% vs. 28%).

 Security information

dangerous mark:T

Hazard category code: 25

Safety instructions: 45

Dangerous goods transport number: UN 2811 6.1 / PG 3

WGK Germany:3

RTECS No:KD4201200

Hazard level: 6.1

Packaging category: III

Customs code: 2934990002

toxicity:LD50i.p.inmice:>200mg/kg(Kino);LChemicalbookD50inmale,femalerats(mg/kg):57.0,23.6i.v.;134,194orally(Ohara)

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