Molecular Formula | C52H79N5O12
|
Molar Mass | 966.21 |
Density | 1.25 |
Melting Point | 100-105°C |
Boling Point | 1016.2±75.0 °C(Predicted) |
Solubility | DMSO, Methanol (Slightly) |
Appearance | Solid |
Color | White to Pale Yellow |
pKa | 10.40±0.70(Predicted) |
Storage Condition | Hygroscopic, -20°C Freezer, Under Inert Atmosphere |
In vitro study | Zotarolimus (ABT-578) is a semisynthetic analog of rapamycin, made by substituting a tetrazole ring for the natural hydroxyl group at position 42 of rapamycin. Zotarolimus can efficiently inhibit the proliferation of smooth muscle cells and endothelial cells, and the IC50 values are 2.9 nM and 2.6 nM, respectively. Zotarolimus has a similar affinity to rapamycin for binding to the immune protein FKBP12 AND also has comparable potency for inhibiting human and rat T cell proliferation in vitro. Zotarolimus inhibited the proliferation of human T cells and rat T cells induced by Con A with IC50 of 7.0 nM and 1337 nM, respectively. |
In vivo study | In a 28-day well-characterized pig model of coronary restenosis, the Zotarolimus-eluting stent effectively reduced intimal hyperplasia. Compared with bare metal stents, Zotarolimus seems to be able to effectively prevent neointimal thickening and reduce late loss from 1.03mm to 0.62mm, it was accompanied by a 47% reduction in TVF (15.4%Driver stent to 8.1%Endeavor stent). Zotarolimus was able to effectively inhibit the adjuvant DTH,EAE, and Cardiac graft rejection with ED50 values of 1.72,1.17, and 3.71 mg/kg/day, respectively. |