Zotarolimus , 95% , 221877-54-9

CAS NO.：221877-54-9

Empirical Formula: C52H79N5O12

Molecular Weight: 966.21

MDL number: MFCD09752954

PRODUCT Properties

• Melting point: 100-105°C
• Boiling point: 1016.2±75.0 °C(Predicted)
• Density: 1.25
• storage temp.: Hygroscopic, -20°C Freezer, Under Inert Atmosphere
• solubility: DMSO, Methanol (Slightly)
• form: Solid
• pka: 10.40±0.70(Predicted)
• color: White to Pale Yellow

Description and Uses

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.

A tetrazole-containing Rapamycin analog as immunomodulator and useful in the treatment of restenosis and immune and autoimmune diseases.

Safety

• Symbol(GHS): GHS07
• Signal word: warning
• Hazard statements: H315-H319-H335
• Precautionary statements: P264-P280-P302+P352-P321-P332+P313-P362-P305+P351+P338-P337+P313-P261-P271-P304+P340-P312-P403+P233-P405-P501
• HS Code: 29349990