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Z-9040 Zotarolimus, >98%

[ABT-578] [40-Epi-(N1-tetrazolyl)-rapamycin]

Z-9040PR

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M.W. 966.21

C₅₂H₇₉N₅O₁₂

[221877-54-9]

Storage: Store at or below -20 ºC. Solubility: Soluble in DMSO. Disposal: A

Zotarolimus (also known as ABT-578) is an analogue of rapamycin (sirolimus) that was designed to have a shorter in vivo half-life than rapamycin. Zotarolimus was found to be comparable in potency for inhibiting in vitro proliferation of both rat and human T cells and mechanistically similar to sirolimus in having high-affinity binding to the immunophilin FKBP12. Chen, Y.W., 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. 49: 228-235 (2007).

In vitro, zotarolimus inhibited FKBP-12 binding (IC50 = 2.8 nM) and potently blocked smooth muscle cell (IC50 = 2.9 nM) and endothelial cell (IC50 = 2.6 nM) proliferation. After 28 days, zotarolimus stents from domestic juvenile swine exhibited less area stenosis (22.4% vs. 35.7%), less neointimal area (1.69 vs. 2.78 mm2), less neointimal thickness (0.25 vs. 0.38 mm), and greater lumen area (6.07 vs. 5.02 mm2) when compared to phosphorylcholine-coated stents. Garcia-Touchard, A., et al. "Zotarolimus-eluting stents reduce experimental coronary artery neointimal hyperplasia after 4 weeks." Eur. Heart J. 27: 988-993 (2006).

Zotarolimus was also designed for use in stents that have phosphorylcholine as a carrier.

Zotarolimus is the active drug in the drug-eluting stents sold under the trade name Endeavor® and ZoMaxx®. NOTE: The zotarolimus sold by LC Laboratories is NOT Endeavor® or ZoMaxx®, and is NOT for human use.

Sold for laboratory or manufacturing purposes only; not for human, veterinary, food, or household use.

This product is offered for R&D use in accordance with (i) 35 USC 271(e)+A13(1) in the U.S.; (ii) Section 69.1 of Japanese Patent Law in Japan; (iii) Section 11, No. 2 of the German Patent Act of 1981 in Germany; (iv) Section 60, Paragraph 5b of the U.K. Patents Act of 1977 in the U.K.; (v) Sections 55.2(1) and 55.2(6) and other common law exemptions of Canadian patent law; (vi) Section 68B of the Patents Act of 1953 in New Zealand together with the amendment of same by the Statutes Amendment Bill of 2002; (vii) such related legislation and/or case law as may be or become applicable in the aforementioned countries; and (viii) such similar laws and rules as may apply in various other countries.

Not available in some countries; not available to some institutions; not available for some uses.

Zotarolimus