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(Synonyms: 佐他莫司; ABT-578; A 179578) 目录号 : GC14224

A macrocyclic lactone immunosuppressant

Zotarolimus(ABT-578) Chemical Structure

Cas No.:221877-54-9

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25mg
¥2,331.00
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5mg
¥924.00
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产品描述

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

Cas No. 221877-54-9 SDF
别名 佐他莫司; ABT-578; A 179578
分子式 C52H79N5O12 分子量 966.21
溶解度 DMF: 15mg/mL,DMSO: 15mg/mL,Ethanol: 20mg/mL,Ethanol:PBS (pH 7.2) (1:3): 0.25mg/mL 储存条件 Store at -20°C
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1 mg 5 mg 10 mg
1 mM 1.035 mL 5.1749 mL 10.3497 mL
5 mM 0.207 mL 1.035 mL 2.0699 mL
10 mM 0.1035 mL 0.5175 mL 1.035 mL
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