上海懋康生物科技有限公司
主營產(chǎn)品: 硫酸諾爾斯菌素,D-熒光素,雷帕霉素 |

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上海懋康生物科技有限公司
主營產(chǎn)品: 硫酸諾爾斯菌素,D-熒光素,雷帕霉素 |
聯(lián)系電話
參考價 | ¥ 248 |
訂貨量 | 1 件 |
更新時間:2024-04-09 16:08:10瀏覽次數(shù):979
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Rapamycin (Sirolimus) 雷帕霉素(西羅莫司)
產(chǎn)品標(biāo)簽
Rapamycin雷帕霉素;Sirolimus西羅莫司;3-MA 3-甲基腺嘌呤;自吞噬抑制劑 Autophagy inhibitor;mTOR;CAS:53123-88-9;
產(chǎn)品信息
產(chǎn)品名稱 | 產(chǎn)品編號 | CAS NO. | 規(guī)格 | 價格(元) |
Rapamycin (Sirolimus) 雷帕霉素(西羅莫司) | MZ0201-10MG | 53123-88-9 | 10mg | 248 |
Rapamycin (Sirolimus) 雷帕霉素(西羅莫司) | MZ0201-50MG | 53123-88-9 | 50mg | 480 |
Rapamycin (Sirolimus) 雷帕霉素(西羅莫司) | MZ0201-100MG | 53123-88-9 | 100mg | 680 |
Rapamycin (Sirolimus) 雷帕霉素(西羅莫司) | MZ0201-500MG | 53123-88-9 | 500mg | 2680 |
Rapamycin (Sirolimus) 雷帕霉素(西羅莫司) | MZ0201-1000MG | 53123-88-9 | 1g | 3980 |
產(chǎn)品描述
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
CAS NO:53123-88-9
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
同義名:Sirolimus, Antibiotic AY 22989, AY 22989, Cypher, RAPA, NSC-226080, Rapamune, SILA 9268A
分子式:C51H79NO13
分子量:914.18
純度:≥98%
外觀:白色至類白色固體
溶解性:溶于DMSO(25mg/ml),乙醇(15mg/ml),幾乎不溶于水
化學(xué)結(jié)構(gòu)圖:
使用方法【源自文獻(xiàn),僅作參考】
文獻(xiàn)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 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℃. 實驗方法(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,Caramés B et al. Autophagy activation by rapamycin reduces severity of experimental osteoarthritis. Ann Rheum Dis. 2012 Apr;71(4):575-81. PMID: 22084394 體內(nèi)研究: 動物模型(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,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 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. 實驗方法(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
雷帕霉素幾乎不溶于水(文獻(xiàn)報道僅2.6µg/ml)。[Simamora P et al. Int J Pharm. 2001 Feb 1;213(1-2):25-9.]
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— —Written/Edited by V. Shallan【版權(quán)歸MKBio懋康所有】
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Rapamycin 雷帕霉素(西羅莫司)/53123-88-9 信號轉(zhuǎn)導(dǎo)研究
Rapamycin 雷帕霉素(西羅莫司)/53123-88-9 信號轉(zhuǎn)導(dǎo)研究