名称 | Zotarolimus |
描述 | Zotarolimus (ABT-578), an analogue of rapamycin, inhibits FKBP-12 (IC50= 2.8 nM). |
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) |
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. |
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). |
体外活性 | 在平滑肌细胞(IC50=2.9 nM)和内皮细胞(IC50=2.6 nM)中,Zotarolimus有效抑制细胞增殖。 |
体内活性 | Zotarolimus 强效抑制剂,对辅助性迟发型超敏反应(DTH)(ED50=1.72 mg/kg/day)、实验性自身免疫性脑炎(EAE)(ED50=1.17 mg/kg/day)、以及心脏移植排斥反应(ED50=3.71 mg/kg/day)表现出显著的抑制作用。 |
存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
溶解度 | Ethanol : 93 mg/mL (96.3 mM) DMSO : 93 mg/mL (96.3 mM) H2O : < 1 mg/mL (insoluble or slightly soluble)
|
关键字 | coronary | ABT 578 | drug-eluting | inhibit | artery | disease | restenosis | Rapamycin | Zotarolimus | ABT578 | immunosuppressant | A-179578 | stents | A179578 | Inhibitor |
相关产品 | α-Hydroxyglutaric Acid Lithium | P-2281 | Capivasertib | Rapamycin | Bimiralisib | L-Leucine | GDC0084 | Tacrolimus | Dihydromyricetin | PI3K/Akt/mTOR-IN-2 | Sapanisertib | (+)-Usnic acid |
相关库 | 经典已知活性库 | 已知活性化合物库 | 激酶抑制剂库 | 抗衰老化合物库 | 药物功能重定位化合物库 | 抗癌临床化合物库 | 抗癌药物库 |