MZ0201-Rapamycin 雷帕霉素（西罗莫司）/53123-88-9 mTOR pathway-生化试剂

产品详情

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

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

CAS NO：53123-88-9
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
同义名：Sirolimus, Antibiotic AY 22989, AY 22989, Cypher, RAPA, NSC-226080, Rapamune, SILA 9268A
分子式：C₅₁H₇₉NO₁₃
分子量：914.18
纯度：≥98%
外观：白色至类白色固体
溶解性：溶于DMSO（25mg/ml），乙醇（15mg/ml），几乎不溶于水
化学结构图：

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

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.]
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。
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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