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| 品牌 | absin | CAS | 221877-54-9 |
|---|---|---|---|
| 分子式 | C52H79N5O12 | 纯度 | 98% |
| 分子量 | 966.21 | 货号 | abs47028251 |
| 规格 | 2mg | 供货周期 | 现货 |
| 主要用途 | is an analogue of rapamycin | 应用领域 | 化工,生物产业,农林牧渔,制药/生物制药,综合 |
Zotarolimus 221877-54-9
| 产品描述 | |
| 描述 | Zotarolimus (ABT-578) is an analogue of rapamycin, and inhibits FKBP-12 binding with IC50 of 2.8 nM. |
| 纯度 | 98% |
| 储存/保存方法 | Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution. |
| 基本信息 | |
| 别名 | 咗他莫司；佐他莫司; ABT-578；A 179578 |
| 外观 | White to Pale Yellow Solid |
| 可溶性/溶解性 | Ethanol : 93 mg/mL (96.25 mM) DMSO : 93 mg/mL (96.25 mM) |
| 生物活性 | |
| 靶点 | FKBP-12 |
| In vitro(体外研究) | 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. |
| In vivo(体内研究) | 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. |
| 研究领域 | |
| 研究领域 | CancerCell cycleCell cycle inhibitorsOther CardiovascularHeartCardiogenesisTranscription factors/regulators Cell CycleCell Cycle InhibitorsOther EpigeneticsDNA / RNADNA Damage & RepairDNA Damage ResponseDNA Damage Recognition MetabolismTypes of diseaseObesity NeuroscienceDevelopment NeuroscienceProcesses Drug DiscoverySmall Molecule DrugLead Compound Discovery |
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