Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Zotarolimus (ABT-578) 是一种免疫抑制剂,是雷帕霉素的衍生物,具有抗增殖活性。它被专门开发作为局部输送支架用于预防冠状动脉再狭窄。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 553 | 现货 | ||
2 mg | ¥ 793 | 现货 | ||
5 mg | ¥ 1,230 | 现货 | ||
10 mg | ¥ 1,830 | 现货 | ||
25 mg | ¥ 3,320 | 现货 | ||
50 mg | ¥ 4,750 | 现货 | ||
100 mg | ¥ 6,620 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,930 | 现货 |
产品描述 | Zotarolimus (ABT-578), an analogue of rapamycin, inhibits FKBP-12 (IC50= 2.8 nM). |
靶点活性 | FKBP12:2.8 nM |
体外活性 | In smooth muscle cell (IC50=2.9 nM)and endothelial cell (IC50=2.6 nM),Zotarolimus effectively inhibits cells proliferation. |
体内活性 | Zotarolimus potently inhibits adjuvant DTH(ED50=1.72 mg/kg/day), EAE(ED50=1.17 mg/kg/day), and cardiac allograft rejection(ED50=3.71 mg/kg/day) . |
激酶实验 | zotarolimus (10 pM-1 μM) in buffer A (2% BSA and 0.2% Tween-20 in D-PBS) is used in the assay of Binding Affinity to FKBP12. |
细胞实验 | Cell proliferation is assayed by measuring tritiated thymidine incorporation in vitro. Human coronary artery cells (hCa) are seeded into tissue culture flasks for expansion and applied to 96-well plates at desired density in complete media (5000 hCaSMC; 10 000 hCaEC). After 2 days, complete media is replaced with incomplete media to synchronize cells and induce G0 state. Two days later, incomplete media are removed and replaced with complete media (serum/growth factors) to induce G0 to G1 transition. Complete media also contain drug at desired concentrations to determine its effects on cell proliferation. On day 7, 3H-thymidine is added to cells to monitor DNA synthesis, and cells are harvested after overnight incorporation of radioactivity. After an incubation period of 72 h, 25 μL (1 μCi/well) of 3H-thymidine are added to each well. The cells are incubated at 37°C for 16-18 h to allow for incorporation of 3H-thymidine into newly synthesized DNA and the cells harvested onto 96-well plates containing bonded glass fibre filters . The filter plates are air-dried overnight, MicroScint-20 (25 μL) added to each filter well and counted. Drug activity is determined by the inhibition of 3H-thymidine incorporation into newly synthesized DNA relative to cells grown in complete media. (Only for Reference) |
动物实验 | Male Sprague-Dawley rats was administrate by intravenous or oral Zotarolimus(2.5 mg/kg)dissolved inethanol: propylene glycol: cremophor EL: D5W vehicle (20: 30: 2: 48, by volume). |
别名 | ABT-578, 佐他莫司, 咗他莫司, A 179578 |
分子量 | 966.21 |
分子式 | C52H79N5O12 |
CAS No. | 221877-54-9 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ethanol: 93 mg/mL (96.3 mM)
DMSO: 93 mg/mL (96.3 mM)
H2O: < 1 mg/mL (insoluble or slightly soluble)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
Ethanol / DMSO | 1 mM | 1.035 mL | 5.1749 mL | 10.3497 mL | 25.8743 mL |
5 mM | 0.207 mL | 1.035 mL | 2.0699 mL | 5.1749 mL | |
10 mM | 0.1035 mL | 0.5175 mL | 1.035 mL | 2.5874 mL | |
20 mM | 0.0517 mL | 0.2587 mL | 0.5175 mL | 1.2937 mL | |
50 mM | 0.0207 mL | 0.1035 mL | 0.207 mL | 0.5175 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Zotarolimus 221877-54-9 PI3K/Akt/mTOR signaling mTOR coronary ABT 578 drug-eluting inhibit artery disease ABT-578 restenosis 佐他莫司 Rapamycin 咗他莫司 ABT578 immunosuppressant A-179578 stents A179578 Inhibitor A 179578 inhibitor