ZOTAROLIMUS
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- Product name: ZOTAROLIMUS
- CAS: 221877-54-9
- MF: C52H79N5O12
- MW: 966.21
- EINECS:
- MDL Number:MFCD09752954
- 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
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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
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
Safety Information
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Description
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.Related product price
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