A macrocyclic lactone immunosuppressant; binds to FKBP12 (IC50 = 2.57 nM); inhibits proliferation of human PBMCs

Zotarolimus – 5 mg

Brand:
Cayman
CAS:
221877-54-9
Storage:
-20
UN-No:
Non-Hazardous - /

Zotarolimus is a macrocyclic lactone immunosuppressant and a derivative of rapamycin (Item No. 13346).{48775,48776} 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).{48776} 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.{48775} Formulations containing zotarolimus have been used in drug-eluting stents in the prevention of restenosis following stent placement.  

 

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Description

A macrocyclic lactone immunosuppressant; binds to FKBP12 (IC50 = 2.57 nM); inhibits proliferation of human PBMCs, rat splenocytes, and human coronary artery smooth muscle cells (IC50s = 7, 1,337, and 0.8 nM, respectively); has immunosuppressive activity in a one-way mixed lymphocyte reaction using human or rat lymphocytes (IC50s = 1.2 and 1,465 nM, respectively); reduces symptom severity in a rat model of EAE (ED50 = 1.17 mg/kg per day); delays cardiac allograft rejection in rats (ED50 = 3.71 mg/kg per day); 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

Formal name: (42S)-42-deoxy-42-(1H-tetrazol-1-yl)-rapamycin

Synonyms:  A-179578|ABT-578

Molecular weight: 966.2

CAS: 221877-54-9

Purity: ≥95% (mixture of isomers)

Formulation: A solid

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