Rapamycin (Sirolimus) 雷帕霉素（西罗莫司）
产品标签
Rapamycin 雷帕霉素；Sirolimus 西罗莫司；3-MA 3-甲基腺嘌呤；自吞噬抑制剂 Autophagy inhibitor；mTOR；CAS：53123-88-9；
产品信息
| 产品名称 | 产品编号 | CAS NO. | 规格 | 价格（元） |
| Rapamycin (Sirolimus) 雷帕霉素（西罗莫司） | MZ0201-10MG | 53123-88-9 | 10mg | 248 |
| Rapamycin (Sirolimus) 雷帕霉素（西罗莫司） | MZ0201-50MG | 53123-88-9 | 50mg | 480 |
| Rapamycin (Sirolimus) 雷帕霉素（西罗莫司） | MZ0201-100MG | 53123-88-9 | 100mg | 680 |
| Rapamycin (Sirolimus) 雷帕霉素（西罗莫司） | MZ0201-500MG | 53123-88-9 | 500mg | 2680 |
| Rapamycin (Sirolimus) 雷帕霉素（西罗莫司） | MZ0201-1000MG | 53123-88-9 | 1g | 3980 |
【温馨提示】：见我司的小分子化合物常见问题-懋康生物。
产品描述
雷帕霉素（Rapamycin），也称西罗莫司（Sirolimus），AY 22989，一种分离自细菌的大环内酯化合物，抗真菌剂和免疫抑制剂。雷帕霉素是一种特异性的mTOR抑制剂，IC50为~0.1nM（HEK293细胞）。与细胞内受体FKBP-12结合形成复合物，之后作用于mTOR中的FRB结构域从而抑制蛋白活性。雷帕霉素处理细胞引起p70 S6激酶的去磷酸化和功能失活（IC50= 50 pM）。还能引起4E-BP1/PHAS1去磷酸化，进而促使其结合并失活eIF4E。雷帕霉素能够阻断蛋白合成和诱导细胞周期停滞在G1期。还能诱导酵母和哺乳动物细胞的自吞噬现象。能驱使人多能干细胞（hPSC）分化成中内胚层和血液祖细胞。
产品特性
1）CAS NO：53123-88-9
2）化学名：(3S,6R,7E,9R,10R,12R,14S,15E,17E,19E,21S,23S,26R,27R,34aS)-9,10,12,13,14,21,22,23,24,25, 26,27,32,33,34,34a-Hexadecahydro-9,27-dihydroxy-3-[(1R)-2-[(1S,3R,4R)-4-hydroxy-3-methoxycyclohexyl]-1-methylethyl]-10,21-dimethoxy-6,8,12,14,20,26-hexamethyl-23,27-epoxy-3H-pyrido[2,1-c][1,4]oxaazacyclohentriacontine-1,5,11,28,29(4H,6H,31H)-pentone
3）同义名：Sirolimus, Antibiotic AY 22989, AY 22989, Cypher, RAPA, NSC-226080,Rapamune, SILA 9268A
4）分子式：C51H79NO13
5）分子量：914.18
6）纯度：≥98%
7）外观：白色至类白色固体
8）溶解性：溶于DMSO（25mg/ml），乙醇（15mg/ml），几乎不溶于水
9）化学结构图：
保存与运输方法
保存：-20ºC干燥保存，至少2年有效。
运输：室温运输。
使用方法【源自文献，仅作参考】
| 文献1，Iwamaru A et al. Silencing mammalian target of rapamycin signaling by small interfering RNA enhances rapamycin-induced autophagy in malignant glioma cells. Oncogene. 2007 Mar 22; 26(13):1840-51. PMID: 17001313
体外研究： 细胞类型（Cell type）：Human malignant glioma U87-MG and A172 cells 药物配制（Preparation）：Rapamycin was dissolved in DMSO to make 1mM stock solution and stored at -20℃. 实验方法（Assay）：Tumor cells were exposed to rapamycin (1, 10 or 100 nm) for 24 or 48 h. The cytotoxic effect of rapamycin was determined using a WST-1 cell proliferation assay. |
| 文献2，Caramés B et al. Autophagy activation by rapamycin reduces severity of experimental osteoarthritis. Ann Rheum Dis. 2012 Apr;71(4):575-81. PMID: 22084394
体内研究： 动物模型（Animal Model）：Experimental osteoarthritis was induced in 2-month-old male C57Bl/6J mice 药物配制（Preparation）：Rapamycin was dissolved in DMSO at 25mg/ml and stored at -20℃. For injection, the stock solution was diluted in phosphate buffered saline (PBS). 注射剂量（Dosages）：Mice received daily intraperitoneal injections of rapamycin at 1 mg/kg body weight/dose in a total injection volume of 0.3 ml for 10 weeks and control animals received the DMSO vehicle at 0.4% in a total injection volume of 0.3 ml. 给药途径（Administration）：Intraperitoneal (i.p.) injection |
| 文献3，Eshleman JS et al. Inhibition of the Mammalian Target of Rapamycin Sensitizes U87 Xenografts to Fractionated Radiation Therapy. Cancer Res. 2002 Dec 15;62(24):7291-7. PMID: 12499272
体外研究： 细胞类型（Cell type）：A172, U87, and U118 malignant glioma cell lines 药物配制（Preparation）：Rapamycin (NSC 226080) was dissolved in ethanol to yield a 5 mg/ml stock solution, which was stored at −20°C. 实验方法（Assay）：Tumor cells were incubated with 0 or 100 nM rapamycin at 37°C for 72 h and then processed in a MTS assay. 体内研究： 动物模型（Animal Model）：8-10-week-old female athymic nude mice by s.c. injection of 2-5 million U87 cells 药物配制（Preparation）：For rapamycin injections, stock rapamycin was diluted first in sterile 10% PEG400/8% ethanol and then in an equal volume of sterile 10% Tween 80 for a final concentration of 20 μg rapamycin/100 μl. Rapamycin was delivered by i.p. injection, and the doses of rapamycin were calculated assuming that all mice weighed 20 g. 给药途径（Administration）：Intraperitoneal (i.p.) injection |
注意事项
1）雷帕霉素几乎不溶于水（文献报道仅2.6µg/ml）。[Simamora P et al. Int J Pharm. 2001 Feb 1;213(1-2):25-9.]
2）本品不是临床药物，只能用于科研用途，不能用于诊断或临床用途。
3）为了您的安全和健康，请穿实验服并戴一次性手套操作。
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— —Written/Edited by V. Shallan【版权归集麒生物/MKBio懋康所有】
