Toggle Nav
Close
  • Menu
  • Setting

Zotarolimus(ABT-578)

Catalog No.
B4786
anti-proliferative drug used exclusively in coronary drug eluting stent
Grouped product items
SizePriceStock Qty
5mg
$130.00
In stock
25mg
$340.00
Ship with 10-15 days

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

Background

Zotarolimus(ABT-578) is an anti-proliferative drug used exclusively in coronary drug eluting stent [1].

Zotarolimus(ABT-578) is an analogue of rapamycin and an anti-proliferative drug. Zotarolimus exhibited high affinity to the immunophilin FKBP12 and inhibited T cells proliferation [1]. Zotarolimus inhibited FKBP-12 binding with IC50 value of 2.8 nM. In human coronary artery cells, zotarolimus inhibited smooth muscle cell (SMC) and endothelial cell (EC) proliferation with IC50 values of 2.9 and 2.6 nM, respectively [2]. In human blood-derived peripheral blood mononuclear cells (PBMC) and rat splenocytes, zotarolimus inhibited Con A-induced human and rat T cell proliferation with IC50 values of 7.0 and 1337 nM respectively in a concentration-dependent way. In lymphocytes derived from humans or rats, zotarolimus inhibited the human and rat mixed lymphocyte reaction (MLR) with IC50 values of 1.2 and 1465 nM respectively in a concentration-dependent way. Also, zotarolimus inhibited human coronary artery smooth muscle cell proliferation induced by growth factor with IC50 value of 0.8 nM [3].

In crossbred juvenile swine, zotarolimus-eluting PC-coated stents induced a lower percent lumen stenosis, less neointimal area, less neointimal thickness and greater lumen area [2]. In a rat adjuvant DTH model mediated by T cell, zotarolimus inhibited the rat adjuvant DTH response with ED50 value of 1.72 mg/kg/day [3].

References:
[1].  Brugaletta S, Burzotta F, Sabaté M. Zotarolimus for the treatment of coronary artery disease: pathophysiology, DES design, clinical evaluation and future perspective. Expert Opin Pharmacother, 2009, 10(6): 1047-1058.
[2].  Garcia-Touchard A, Burke SE, Toner JL, et al. Zotarolimus-eluting stents reduce experimental coronary artery neointimal hyperplasia after 4 weeks. Eur Heart J, 2006, 27(8): 988-993.
[3].  Chen YW, Smith ML, Sheets M, et al. Zotarolimus, a novel sirolimus analogue with potent anti-proliferative activity on coronary smooth muscle cells and reduced potential for systemic immunosuppression. J Cardiovasc Pharmacol, 2007, 49(4): 228-235.

Chemical Properties

StorageDesiccate at -20°C
M.Wt966.21
Cas No.221877-54-9
FormulaC52H79N5O12
Solubilityinsoluble in EtOH; ≥24.75 mg/mL in H2O; ≥26.75 mg/mL in DMSO
SDFDownload SDF
Shipping ConditionEvaluation sample solution: ship with blue ice. All other available sizes: ship with RT, or blue ice upon request.
General tipsFor obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. Stock solution can be stored below -20°C for several months.

Quality Control

Quality Control & MSDS

View current batch:

Chemical structure

Zotarolimus(ABT-578)