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Rapamycin

产品编号 T1537Cas号 53123-88-9
别名 西罗莫司, 雷帕霉素, Sirolimus, NSC-2260804, AY 22989

Rapamycin (AY 22989) 属于大环内酯类天然产物,是一种 mTOR 抑制剂,具有特异性(HEK293 细胞:IC50=0.1 nM)。Rapamycin 具有免疫抑制活性,并能诱导自噬。

Rapamycin

Rapamycin

纯度: 99.03%
产品编号 T1537 别名 西罗莫司, 雷帕霉素, Sirolimus, NSC-2260804, AY 22989Cas号 53123-88-9

Rapamycin (AY 22989) 属于大环内酯类天然产物,是一种 mTOR 抑制剂,具有特异性(HEK293 细胞:IC50=0.1 nM)。Rapamycin 具有免疫抑制活性,并能诱导自噬。

规格价格库存数量
1 mg¥ 133现货
5 mg¥ 283现货
10 mg¥ 455现货
25 mg¥ 619现货
50 mg¥ 892现货
100 mg¥ 1,230现货
200 mg¥ 1,850现货
500 mg¥ 3,150现货
1 mL x 10 mM (in DMSO)¥ 490现货
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纯度:99.03%
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产品介绍

生物活性
产品描述
Rapamycin (AY 22989) is a natural product of macrolides, an mTOR inhibitor with specificity (HEK293 cells: IC50=0.1 nM). Rapamycin has immunosuppressive activity and induces autophagy.
靶点活性
mTOR:0.1 nM (HEK293 cells)
体外活性
方法:正常人肾上皮细胞 HRECs 用 Rapamycin (0.01-1000 nmol/L) 处理 6 天,使用 MTT 方法检测细胞生长抑制情况。
结果:Rapamycin 剂量依赖性地抑制 HRECs 细胞生长,在10 nmol/L 的浓度下,细胞活力降低了40%。[1]
方法:人宫颈癌细胞 HeLa 和人前列腺癌细胞 PC3 用 Rapamycin (100 nM) 处理 0.5-24 h,使用 Immunoprecipitation 方法检测靶点蛋白表达水平。
结果:Rapamycin 对 mTOR、raptor 和 rictor 的表达水平影响不大,在 0.5 h 内显著降低了与 mTOR 结合的 raptor,在 24 h 时降低了与 mTOR 结合的 rictor。Rapamycin 长期处理细胞抑制 mTORC2 的组装。[2]
方法:人血管内皮细胞用 Rapamycin (1-100 ng/mL) 处理 48 h,使用 Wound-healing 方法检测细胞迁移情况。
结果:Rapamycin 剂量依赖性地抑制人血管内皮细胞的迁移能力。[3]
体内活性
方法:为研究 Rapamycin 寿命的影响,将 Rapamycin (8 mg/kg in DMSO+5% PEG-400+5% Tween-80) 腹腔注射给 20–21 个月大的 C57BL/6J 小鼠,每天一次,持续三个月。
结果:Rapamycin 治疗 3 个月足以将中年小鼠的预期寿命提高60%,并改善其健康寿命。[4]
方法:为确定 Rapamycin 治疗癫痫的合适剂量,将 Rapamycin (0.1-3 mg/kg in 4% ethanol+5% Tween 80+5% PEG 400) 腹腔注射给 Sprague-Dawley 大鼠,每天一次,持续四周。
结果:只有 1.0 mg/kg 和 3.0 mg/kg Rapamycin 抑制 p-S6。用 0.1 和 0.3 mg/kg Rapamycin 处理的大鼠没有明显的不良反应,而用 1.0 和 3.0 mg/kg Rapamycin 处理的大鼠的身体、脾脏和胸腺重量显著降低,表现出认知障碍和焦虑。Rapamycin 剂量不能抑制 mTOR 治疗癫痫而不引起任何副作用,但 1 mg/kg 可能是年轻大鼠抑制 mTOR 的最佳剂量,副作用相对较少。[5]
激酶实验
HEK293 cells were plated at 2-2.5 × 10^5 cells per well of a 12-well plate and serum-starved for 24 h in DMEM only. Cells were mock-treated or treated with rapamycin (0.05-50 nM), iRap (0.5-500 nM), or AP21967 (0.5-500 nM) for 15 minutes at 37 °C. Serum was added to a final concentration of 20% for 30 minutes at 37 °C. Cells were lysed as described and cell lysates were separated by SDS-PAGE. Resolved proteins were transferred to a PVDF membrane and immunoblotted with a phosphospecific primary antibody against Thr389 of p70 S6 kinase. Data were analyzed using ImageQuant and KaleidaGraph [1].
细胞实验
To determine the effects of rapamycin and rapamycin plus LY294002 or UCN-01 on tumor cells, we determined cell viability after the treatments. We used a trypan blue dye exclusion assay as described previously. Tumor cells in exponential growth were harvested and seeded at 5 × 10^3 cells per well (0.1 mL) in 96-well flat-bottomed plates and incubated overnight at 37°C. The cells were then incubated for 72 hours with or without rapamycin or with rapamycin plus LY294002 or UCN-01. After the cells were collected by trypsinization, they were stained with trypan blue, and the viable cells in each well were counted. The viability of the untreated cells (the control) was considered 100%. Survival fractions were calculated from the mean cell viability of the treated cells [3].
动物实验
Animals were randomized to treatment or vehicle groups so that the mean starting body weights of each group were equal. Drug treatment began on the day of surgery or on the first day of reloading after the 14-day suspension. Rapamycin was delivered once daily by intraperitoneal injection at a dose of 1.5 mg/kg, dissolved in 2% carboxymethylcellulose. CsA was delivered once daily by subcutaneous injection at a dose of 15 mg/kg, dissolved in 10% methanol and olive oil. FK506 was delivered once daily via subcutaneous injection at a dose of 3 mg/kg, dissolved in 10% ethanol, 10% cremophor and saline [4].
别名西罗莫司, 雷帕霉素, Sirolimus, NSC-2260804, AY 22989
化学信息
分子量914.17
分子式C51H79NO13
CAS No.53123-88-9
储存&溶解度
存储Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
溶解度信息
Ethanol: 100 mg/mL (109 mM), Sonication is recommended.
H2O: Insoluble
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 10 mg/mL (10.94 mM), Please add co-solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately.
DMSO: 100 mg/mL (109 mM), Sonication is recommended.
溶液配制表
10% DMSO+40% PEG300+5% Tween 80+45% Saline/Ethanol/DMSO
1mg5mg10mg50mg
1 mM1.0939 mL5.4694 mL10.9389 mL54.6944 mL
5 mM0.2188 mL1.0939 mL2.1878 mL10.9389 mL
10 mM0.1094 mL0.5469 mL1.0939 mL5.4694 mL
Ethanol/DMSO
1mg5mg10mg50mg
20 mM0.0547 mL0.2735 mL0.5469 mL2.7347 mL
50 mM0.0219 mL0.1094 mL0.2188 mL1.0939 mL
100 mM0.0109 mL0.0547 mL0.1094 mL0.5469 mL

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  • 稀释 计算器
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体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法:
TargetMol | Animal experiments比如您的给药剂量是 10 mg/kg ,每只动物体重 20 g ,给药体积 100 μLTargetMol | Animal experiments 一共给药动物 10 只 ,您使用的配方为 5% TargetMol | reagent DMSO+ 30%PEG300+ 5%Tween 80 + 60% ddH2O. 那么您的工作液浓度为 2 mg/mL
母液配置方法: 2 mg 药物溶于 50 μLDMSOTargetMol | reagent ( 母液浓度为 40 mg/mL ), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:50μLDMSOTargetMol | reagent 母液,添加 300 μLPEG300TargetMol | reagent 混匀澄清,再加 50μLTween 80, 混匀澄清,再加 600μLddH2OTargetMol | reagent 混匀澄清

以上为“体内实验配液计算器”的使用方法举例,并不是具体某个化合物的推荐配制方式,请根据您的实验动物和给药方式选择适当的溶解方案。

1 请输入动物实验的基本信息
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2 请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
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剂量转换

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