221877-54-9

Basic information

• Product Name: ZOTAROLIMUS
• Synonyms: ZOTAROLIMUS;(42S)-42-Deoxy-42-(1H-tetrazol-1-yl)rapamycin;A 179578;ABT 578;Rapamycin, 42-deoxy-42-(1H-tetrazol-1-yl)-, (42S)-;Unii-H4gxr80ize;ZotaroliMus, >90%;42-(1-Tetrazolyl)rapamycin
• CAS NO: 221877-54-9
• Molecular Formula: C52H79N5O12
• Molecular Weight: 966.219
• Product Categories: Intermediates & Fine Chemicals;Pharmaceuticals;Chiral Reagents;Heterocycles;Inhibitors
• Mol File: 221877-54-9.mol
• Article Data: 0

Chemical Properties

• Melting Point: 100-105°C
• Boiling Point: 1016.2°Cat760mmHg
• Flash Point: 568.4°C
• Appearance: /
• Density: 1.25
• Storage Temp.: Hygroscopic, -20°C Freezer, Under Inert Atmosphere
• Solubility: DMSO, Methanol (Slightly)
• PKA: 10.40±0.70(Predicted)
• CAS DataBase Reference: ZOTAROLIMUS(CAS DataBase Reference)
• NIST Chemistry Reference: ZOTAROLIMUS(221877-54-9)
• EPA Substance Registry System: ZOTAROLIMUS(221877-54-9)

Safety Data

• Hazardous Substances Data: 221877-54-9(Hazardous Substances Data)

Usage

Description

Zotarolimus, a semi-synthetic macrocyclic lactone derivative of rapamycin, is an immunosuppressant with potent immunomodulatory properties. It is characterized by its pale yellow solid appearance and has been extensively studied, with over 200 citations in the literature. Zotarolimus binds to the receptor protein FKBP12, forming a complex that inhibits the interaction with target proteins, thus exerting its immunosuppressive effects.

Uses

Used in Pharmaceutical Industry:
Zotarolimus is used as an immunomodulator for the treatment of restenosis and immune and autoimmune diseases. It demonstrates immunosuppressive activity in various cell types, including human peripheral blood mononuclear cells (PBMCs), rat splenocytes, and human coronary artery smooth muscle cells. It also reduces symptom severity in a rat model of experimental autoimmune encephalomyelitis (EAE) and delays cardiac allograft rejection in rats.
Used in Cardiovascular Applications:
Zotarolimus is used as an agent to inhibit neointimal formation and reduce stenosis in pig coronary arteries. It is applied at 10 μg/mm to stainless steel balloon expandable stents with phosphorylcholine in a model of restenosis, which helps in the prevention of restenosis following stent placement.
Used in Drug-Eluting Stents:
Formulations containing zotarolimus are used in drug-eluting stents to prevent restenosis after stent placement. The drug's less bioavailable profile, due to its structural change, is a preferred characteristic for this application, as it allows for controlled release and sustained therapeutic effects.