ZOTAROLIMUS

Bezeichnung:ZOTAROLIMUS

CAS-Nr221877-54-9

Englisch Name:ZOTAROLIMUS

CBNumberCB21011766

SummenformelC52H79N5O12

Molgewicht966.21

MOL-Datei221877-54-9.mol

ZOTAROLIMUS physikalisch-chemischer Eigenschaften

Schmelzpunkt	100-105°C
Siedepunkt	1016.2±75.0 °C(Predicted)
Dichte	1.25
storage temp.	Hygroscopic, -20°C Freezer, Under Inert Atmosphere
Löslichkeit	DMSO, Methanol (Slightly)
Aggregatzustand	Solid
pka	10.40±0.70(Predicted)
Farbe	White to Pale Yellow

Sicherheit

HS Code

29349990

ZOTAROLIMUS Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung
Zotarolimus is a macrocyclic lactone immunosuppressant and a derivative of rapamycin . It binds to FKBP prolyl isomerase 1A (FKBP12; IC₅₀ = 2.57 nM) and inhibits proliferation of human peripheral blood mononuclear cells (PBMCs), rat splenocytes, and human coronary artery smooth muscle cells (IC₅₀s = 7, 1,337, and 0.8 nM, respectively). Zotarolimus has immunosuppressive activity in a one-way mixed lymphocyte reaction using human or rat lymphocytes (IC₅₀s = 1.2 and 1,465 nM, respectively). It also reduces symptom severity in a rat model of experimental autoimmune encephalomyelitis (EAE; ED₅₀ = 1.17 mg/kg per day) and delays cardiac allograft rejection in rats (ED₅₀ = 3.71 mg/kg per day). Zotarolimus inhibits neointimal formation and reduces stenosis in pig coronary arteries when applied at 10 μg/mm to stainless steel balloon expandable stents with phosphorylcholine in a model of restenosis. Formulations containing zotarolimus have been used in drug-eluting stents in the prevention of restenosis following stent placement.
Chemische Eigenschaften
Pale Yellow Solid
Verwenden
A tetrazole-containing Rapamycin analog as immunomodulator and useful in the treatment of restenosis and immune and autoimmune diseases.
Verwenden
Zotarolimus is a semi-synthetic macrocyclic lactone prepared from rapamycin by preparation of the 42-triflate ester, followed by displacement with tetrazole and purification of the two isomeric products. This structural change affords a less bioavailable product, a preferred profile for some applications. Like all tacrolimus analogues, zotarolimus binds to a receptor protein (FKBP12). The complex then binds to preventing it from interacting with target proteins. Zotarolimus is extensively cited in the literature with over 200 citations.
Definition
ChEBI: Zotarolimus is a macrolide and a lactam.

ZOTAROLIMUS Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

221877-54-9, ZOTAROLIMUS Verwandte Suche:

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