切换导航

Zotarolimus(ABT-578)

现货
Catalog No.
B4786
专用于冠脉药物洗脱支架的抗增殖药物
组合的产品项目
规格价格库存 数量
5mg
¥ 1,300.00
现货
25mg
¥ 3,400.00
现货

电话: 021-55669583

邮箱: sales@apexbio.cn

全球经销商

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
SolubilitySoluble in DMSO
SDFDownload SDF
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

质量控制

化学结构

Zotarolimus(ABT-578)