Basic information Safety Supplier Related
ChemicalBook >  Product Catalog >  Biochemical Engineering >  Inhibitors >  PI3K / Akt / mTOR >  mTOR inhibitors >  ZOTAROLIMUS

ZOTAROLIMUS

Basic information Safety Supplier Related

ZOTAROLIMUS Basic information

Product Name:
ZOTAROLIMUS
Synonyms:
  • ZOTAROLIMUS
  • (42S)-42-Deoxy-42-(1H-tetrazol-1-yl)rapamycin
  • A 179578
  • ABT 578
  • ABT-578;A-179578;ABT578;A179578;ABT 578;A 179578
  • CS-1162
  • Rapamycin, 42-deoxy-42-(1H-tetrazol-1-yl)-, (42S)-
  • Unii-H4gxr80ize
CAS:
221877-54-9
MF:
C52H79N5O12
MW:
966.21
Product Categories:
  • Inhibitors
  • Chiral Reagents
  • Intermediates & Fine Chemicals
  • Pharmaceuticals
  • Heterocycles
Mol File:
221877-54-9.mol
More
Less

ZOTAROLIMUS Chemical 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
pka
10.40±0.70(Predicted)
CAS DataBase Reference
221877-54-9
More
Less

Safety Information

HS Code 
29349990
More
Less

ZOTAROLIMUS Usage And Synthesis

Description

Zotarolimus is a macrocyclic lactone immunosuppressant and a derivative of rapamycin (Item No. 13346). 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.

Chemical Properties

Pale Yellow Solid

Uses

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.

Uses

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

ZOTAROLIMUSSupplier

Shanghai hongqu biomedical technology co. LTD Gold
Tel
Email
hongquchem@qq.com
J & K SCIENTIFIC LTD.
Tel
010-82848833- ;010-82848833
Email
jkinfo@jkchemical.com;market6@jkchemical.com
Chembest Research Laboratories Limited
Tel
021-20908456
Email
sales@BioChemBest.com
LGM Pharma
Tel
1-(800)-881-8210
Email
inquiries@lgmpharma.com
Chemsky(shanghai)International Co.,Ltd.
Tel
021-50135380
Email
shchemsky@sina.com