Rapamycin (Sirolimus) 雷帕霉素

产品简介：

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：

保存条件: 

-20ºC干燥保存，至少2年有效。

产品使用：【源自文献，仅作参考】

文献1:

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:

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:

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）。

2.      为了您的安全和健康，请穿实验服并戴一次性手套操作。