Tacrolimus Monohydrate

Bezeichnung:Tacrolimus Monohydrate

CAS-Nr109581-93-3

Englisch Name:Tacrolimus Monohydrate

CBNumberCB4772400

SummenformelC44H71NO13

Molgewicht822.05

MOL-Datei109581-93-3.mol

Tacrolimus Monohydrate physikalisch-chemischer Eigenschaften

Schmelzpunkt	127-129°
alpha	D23 -84.4° (c = 1.02 in chloroform)
storage temp.	-20°C
Löslichkeit	DMSO: soluble20mg/mL
Aggregatzustand	powder
Farbe	White to Almost white
Merck	14,9025
InChIKey	NWJQLQGQZSIBAF-MLAUYUEBSA-N

Sicherheit

Kennzeichnung gefährlicher	T
R-Sätze:	25
S-Sätze:	45
RIDADR	UN 2811 6.1/PG 3
WGK Germany	3
RTECS-Nr.	KD4201200
HazardClass	6.1
PackingGroup	III
HS Code	2934990002
Toxizität	LD50 i.p. in mice: >200 mg/kg (Kino); LD50 in male, female rats (mg/kg): 57.0, 23.6 i.v.; 134, 194 orally (Ohara)

Gefahreninformationscode (GHS)

Tacrolimus Monohydrate Chemische Eigenschaften,Einsatz,Produktion Methoden

R-Sätze Betriebsanweisung:
R25:Giftig beim Verschlucken.
S-Sätze Betriebsanweisung:
S45:Bei Unfall oder Unwohlsein sofort Arzt zuziehen (wenn möglich, dieses Etikett vorzeigen).
Verwenden
immune suppressant, antifungal
Verwenden
FK-506 monohydrate (Tacrolimus Monohydrate) has been used:
- as an immunosuppressive agent in coculture medium to study the effect of immunologic reaction
- as a calcineurin inhibitor, in anhydrous Me₂SO solution
- to treat retinal pigment epithelial cells to measure possible cytotoxicity
Definition
ChEBI: A hydrate that is the monohydrate form of tacrolimus.
Biologische Aktivität
Potent calcineurin (protein phosphatase 2B) inhibitor that requires FK 506-binding protein 12 (FKBP12) for activity (IC 50 = 3 nM). Inhibits secretion of IL-1, IL-2 (IC 50 = 1 nM), IL-3, IL-4, IL-6 (IC 50 = 35 nM), GM-CSF, TNF α (IC 50 = 10 nM), IFN γ and Myc from activated T-cells in vitro . Exhibits potent immunosuppressive, neuroprotective and anticonvulsant activity in vivo .
Biochem/physiol Actions
FK-506 also appears to inhibit Na+/Ca2+ exchange. FK-506 and its derivatives demonstrate significant neurodegenerative activity. This property seems to arise via different mechanisms. FK-506 is also useful in treating ophthalmologic complications such as corneal graft rejection, uveoretinitis and allergen induced conjunctivitis.
Sicherheitsprofil
A poison by ingestion and intravenous routes. When heated to decomposition it emits toxic vapors of NOx.
in vitro
Tacrolimus monohydrate (FK506 monohydrate; Fujimycin monohydrate; FR900506 monohydrate) inhibits calcium-dependent events, such as IL-2 gene transcription, NO synthase activation, cell degranulation, and apoptosis. Tacrolimus also potentiates the actions of glucocorticoids and progesterone by binding to FKBPs contained within the hormone receptor complex, preventing degradation. The agent may enhance the expression of the TGFβ-1 gene in a fashion analogous to that demonstrated for CsA. T cell proliferation in response to ligation of the T cell receptor is inhibited by Tacrolimus. Treatment with a low concentration of Tacrolimus (FK506,10 μg/L) does not significantly affect the proliferation of MH3924A cells (P=0.135). Upon treatment with higher concentrations of Tacrolimus (100-1,000 μg/L), the proliferation of MH3924A cells is significantly enhanced (P<0.01). Treatment with AMD3100 at any concentration (10, 50 or 100 μg/L) has no obvious effect on MH3924A cell proliferation (P>0.05). However, when different concentrations of AMD3100 are combined with 100 μg/L Tacrolimus, the in vitro proliferation of MH3924A cells is increased (P<0.01).

Tacrolimus Monohydrate Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

109581-93-3, Tacrolimus Monohydrate Verwandte Suche:

Send Inquriy