雷帕霉素

Rapamycin (Sirolimus) 

產(chǎn)品簡(jiǎn)介：

雷帕霉素（Rapamycin），也稱西羅莫司（Sirolimus），AY 22989，一種分離自細(xì)菌的大環(huán)內(nèi)酯化合物，抗真菌劑和免疫抑制劑。雷帕霉素是一種特異性的mTOR抑制劑，IC50為~0.1nM（HEK293細(xì)胞）。與細(xì)胞內(nèi)受體FKBP-12結(jié)合形成復(fù)合物，之后作用于mTOR中的FRB結(jié)構(gòu)域從而抑制蛋白活性。雷帕霉素處理細(xì)胞引起p70 S6激酶的去磷酸化和功能失活（IC50= 50 pM）。還能引起4E-BP1/PHAS1去磷酸化，進(jìn)而促使其結(jié)合并失活eIF4E。雷帕霉素能夠阻斷蛋白合成和誘導(dǎo)細(xì)胞周期停滯在G1期。還能誘導(dǎo)酵母和哺乳動(dòng)物細(xì)胞的自吞噬現(xiàn)象。能驅(qū)使人多能干細(xì)胞（hPSC）分化成中內(nèi)胚層和血液祖細(xì)胞。

產(chǎn)品特性：

1）CAS NO：53123-88-9

2）化學(xué)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）同義名：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）純度：≥98%

7）外觀：白色至類白色固體

8）溶解性：溶于DMSO（25mg/ml），乙醇（15mg/ml），幾乎不溶于水

9）化學(xué)結(jié)構(gòu)圖：

保存條件: 

-20oC干燥保存，至少2年有效。

產(chǎn)品使用：【源自文獻(xiàn)，僅作參考】

文獻(xiàn)1:

體外研究：

細(xì)胞類型（Cell type）：Human malignant glioma U87-MG and A172 cells

藥物配制（Preparation）：Rapamycin was dissolved in DMSO to make 1mM stock solution and stored at -20℃.

實(shí)驗(yàn)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.

文獻(xiàn)2:

體內(nèi)研究：

動(dòng)物模型（Animal Model）：Experimental osteoarthritis was induced in 2-month-old male C57Bl/6J mice

藥物配制（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).

注射劑量（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.

給藥途徑（Administration）：Intraperitoneal (i.p.) injection

文獻(xiàn)3:

體外研究：

細(xì)胞類型（Cell type）：A172, U87, and U118 malignant glioma cell lines

藥物配制（Preparation）：Rapamycin (NSC 226080) was dissolved in ethanol to yield a 5 mg/ml stock solution, which was stored at ?20°C.

實(shí)驗(yàn)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.

體內(nèi)研究：

動(dòng)物模型（Animal Model）：8-10-week-old female athymic nude mice by s.c. injection of 2-5 million U87 cells

藥物配制（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. 

給藥途徑（Administration）：Intraperitoneal (i.p.) injection

注意事項(xiàng)：

1.      雷帕霉素幾乎不溶于水（文獻(xiàn)報(bào)道僅2.6μg/ml）。

2.      為了您的安全和健康，請(qǐng)穿實(shí)驗(yàn)服并戴一次性手套操作。