| 货号 | 16158-500ug |
| 描述 | Rapamycin (Item No. 13346) is a natural macrolide immunosuppressant that activates mTORC1. Seco Rapamycin (sodium salt) is a nonenzyme-dependent degradation product of rapamycin (Item No. 13346) resulting from ester hydration followed by dehydration.1 It has less than 4% of the potency of rapamycin in a thymocyte proliferation assay.1 Rapamycin quickly degrades to two ring-opened products, including seco rapamycin, in the cytoplasm or in homogenates of Caco-2 cells.2 Like rapamycin, seco rapamycin is secreted from cells by P-glycoprotein and metabolized to a common dihydro species.3 While seco rapamycin poorly activates mTOR, it mimics rapamycin in its ability to inhibit the proteasome.4 |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Wang, C.P.,Chan, K.W.,Schiksnis, R.A., et al. High performance liquid chromatographic isolation, spectroscopic characterization, and immunosuppressive activities of two rapamycin degradation products. J.Liq.Chromatogr. 17(16), 3383-3392 (1994). 2.Paine, M.F.,Leung, L.Y.,Lim, H.K., et al. Identification of a novel route of extraction of sirolimus in human small intestine: Roles of metabolism and secretion. Journal of Pharmacology and Experimental Therapeutics 301(1), 174-186 (2002). 3.Paine, M.F.,Leung, L.Y. and Watkins, P.B. New insights into drug absorption: Studies with sirolimus. Therapeutic Drug Monitoring 26(5), 463-467 (2004). 4.Osmulski, P.A. and Gaczynska, M. Rapamycin allosterically inhibits the proteasome. Molecular Pharmacology 84(1), 104-113 (2013). | |
| 运输条件 | Wet ice in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥85% |
| 计算分子量 | 936.2 |
| 分子式 | C51H79NO13 • Na |
| CAS号 | 148554-65-8 |
| 稳定性 | ≥ 2 years |
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