Zotarolimus (ABT-578) is an analogue of rapamycin, and inhibits FKBP-12 binding with IC50 of 2.8 nM.

98%

Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.

DMSO:100 mg/mL (103.49 mM)

FKBP-12

Zotarolimus (ABT-578) is a semi-synthetic analogue of rapamycin, made by substituting a tetrazole ring for the native hydroxyl group at position 42 in rapamycin. Zotarolimus is highly effective in inhibiting both smooth muscle cell and endothelial cell proliferation, with IC50 values of 2.9 nM and 2.6 nM, respectively. Zotarolimus is mechanistically similar to sirolimus in having high-affinity binding to the immunophilin FKBP12 and comparable potency for inhibiting in vitro proliferation of both human and rat T cells. Zotarolimus inhibits Con A-induced human T cells and rat T cells proliferation with IC50 of 7.0 nM and 1337 nM respectively.

Zotarolimus-eluting stents effectively reduce neointima formation in a 28-day, well-characterized swine model of coronary artery restenosis. Zotarolimus appears effective in preventing neointimal thickening, reducing late loss from 1.03 to 0.62 mm with a 47% reduction in TVF compared with bare metal stents (15.4% with the Driver stent to 8.1% with the Endeavor stent). Zotarolimus is efficacious in suppressing adjuvant DTH, EAE, and cardiac allograft rejection with ED50 values of 1.72, 1.17, and 3.71 mg/kg/day, respectively.

1. Garcia-Touchard A, et al. Eur Heart J, 2006, 27(8), 988-993.

2. Chen YW, et al. J Cardiovasc Pharmacol, 2007, 49(4), 228-235.

1. Garcia-Touchard A, et al. Eur Heart J, 2006, 27(8), 988-993.

2. Chen YW, et al. J Cardiovasc Pharmacol, 2007, 49(4), 228-235.