| 產(chǎn)品描述： | Zotarolimus, an analogue of rapamycin, inhibits FKBP-12 (IC50= 2.8 nM). |
| 靶點(diǎn)： |
mTOR |
| 體內(nèi)研究： |
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) |
| 細(xì)胞實(shí)驗(yàn)： |
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 g |
| 動物實(shí)驗(yàn)： |
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). |
| 參考文獻(xiàn)： |
1.Chen YW, et al. J Cardiovasc Pharmacol, 2007, 49(4), 228-235. 2.Garcia-Touchard A, et al. Eur Heart J, 2006, 27(8), 988-1993. |
| 溶解性： |
Ethanol:93 mg/mL (96.3 mM) H2O:<1 mg/mL DMSO:93 mg/mL (96.3 mM) |
| 保存條件： |
2-8℃ |
| 配置溶液濃度參考： |
|
1mg |
5mg |
10mg |
| 1 mM |
1.035 ml |
5.175 ml |
10.35 ml |
| 5 mM |
0.207 ml |
1.035 ml |
2.07 ml |
| 10 mM |
0.103 ml |
0.517 ml |
1.035 ml |
| 50 mM |
0.021 ml |
0.103 ml |
0.207 ml |
|
| 注意： |
部分產(chǎn)品我司僅能提供部分信息，我司不保證所提供信息的權(quán)威性，僅供客戶參考交流研究之用。 |
上海工商
危險品化學(xué)品經(jīng)營許可證（不帶存儲）
營業(yè)執(zhí)照(三證合一)
北京