1. PI3K/Akt/mTOR Autophagy Apoptosis Immunology/Inflammation Anti-infection Metabolic Enzyme/Protease
  2. mTOR FKBP Fungal Autophagy Endogenous Metabolite Antibiotic Bacterial
  3. Rapamycin

Rapamycin  (Synonyms: 雷帕霉素; 西罗莫司; Sirolimus; AY-22989)

目录号: HY-10219 纯度: 99.94%
COA 产品使用指南

Rapamycin (Sirolimus) 是一种有效且特异性的 mTOR 抑制剂,作用于 HEK293 细胞,抑制 mTORIC50 为 0.1 nM。Rapamycin 与 FKBP12 结合且抑制 mTORC1。Rapamycin 还是一种自噬 (autophagy) 激活剂,免疫抑制剂。

MCE 的所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

Rapamycin Chemical Structure

Rapamycin Chemical Structure

CAS No. : 53123-88-9

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10 mM * 1 mL in DMSO ¥605
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5 mg ¥343
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10 mg ¥550
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25 mg ¥750
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50 mg ¥1100
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100 mg ¥1500
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500 mg ¥3800
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Top Publications Citing Use of Products

MCE 顾客使用本产品发表的 722 篇科研文献

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    Rapamycin purchased from MCE. Usage Cited in: J Hazard Mater. 2023 Jul 5,453,131354.

    Rapamycin (50 nM; 24 h) efficiently inhibits the Cobalt-induced hyperphosphorylation of Tau in Ser262 and Thr181, when in H4 cells.

    Rapamycin purchased from MCE. Usage Cited in: PLoS Pathog. 2023 Mar 27;19(3):e1011295.  [Abstract]

    Rapamycin (100 nM; 24 h) increases PRRSV replication in Marc-145 cells.

    Rapamycin purchased from MCE. Usage Cited in: Cancer Cell Int. 2023 Apr 16;23(1):68.  [Abstract]

    Rapamycin (2.5 mM; 24 h) ignificantly reverses the PCK1-sh-induced decreased expression of LC3B-II in SW480-sh cells.

    Rapamycin purchased from MCE. Usage Cited in: Cell Death Dis. 2020 Jun 12;11(6):454.  [Abstract]

    Immunofluorescence staining of p62 is conducted in HSC-T6 cells. G-Rg3 pretreatment with 16 μM and Ra are conducted with 100 or 200 nM.

    Rapamycin purchased from MCE. Usage Cited in: Nature. 2018 Jun;558(7711):540-546.  [Abstract]

    Western blot and quantification of P-AKT (Ser473) and P-S6RP in the liver, heart and muscle, respectively, of PIK3CAWT and PIK3CACAGG-CreER mice treated with vehicle or Rapamycin directly after Cre induction.

    Rapamycin purchased from MCE. Usage Cited in: Acta Biomater. 2018 Nov;81:278-292.  [Abstract]

    Evident LC3 turnover and increased level of Atg5 are found upon Rapamycin treatment, which indicate significant autophagy activation.

    Rapamycin purchased from MCE. Usage Cited in: Int J Cancer. 2018 Aug 15;143(4):931-943.  [Abstract]

    H1975 cells are pretreated with Rapamycin (100 nM) for 1 h and then cells are exposed to IFN-γ (100 U/mL). Phosphorylation of AKT, S6, 4E-BP1 are analyzed by western blotting.

    Rapamycin purchased from MCE. Usage Cited in: Sci Rep. 2018 Mar 7;8(1):4108.  [Abstract]

    L02 cells exposed to PA (200 μM) with different concentrations of Rapamycin (Rapa) or Chloroquine (CQ) for 24 h. Palmitate (PA) induced higher protein expression of LC3 II/I and p62 compared with control as indicated by western blot.

    Rapamycin purchased from MCE. Usage Cited in: Acta Biochim Biophys Sin (Shanghai). 2018 Feb 1;50(2):144-155.  [Abstract]

    Raw264.7 macrophages treated without or with Rapamycin (1 μΜ) or Chloroquine (20 μΜ) for 48 h. Western blot shows the protein expression levels of Atg5, Beclin1, LC3, and p62/SQSMT1.

    Rapamycin purchased from MCE. Usage Cited in: Pharmacol Biochem Behav. 2019 Feb;177:1-11.  [Abstract]

    Effect of treatment with Rapamycin, trehalose, or their combination on tyrosine hydroxylase (TH) expression in the striatum in MPTP-induced mouse model of Parkinson’s disease.

    Rapamycin purchased from MCE. Usage Cited in: Pharmacol Biochem Behav. 2019 Feb;177:1-11.  [Abstract]

    Effect of treatment with Rapamycin, trehalose, or their combination on autophagy activity measured by quantified immunoreactivity of LC3-II in the s. nigra. MPTP is administered at the dose of 20 mg/kg (i.p., daily) for 4 days to induce PD-like pathology.

    Rapamycin purchased from MCE. Usage Cited in: Biotechnol Appl Biochem. 2018 Sep;65(5):665-671.  [Abstract]

    The mTOR inhibitor Rapamycin augments the autophagy induced by GEM. (A, B) Beclin-1 and LC3B expression is analyzed by western blot after treatment of the cells with GEM (5 μM) and Rapamycin (0, 1, and 2.5 μM) for 48 (A) or 72 (B) h.

    Rapamycin purchased from MCE. Usage Cited in: PeerJ. 2018 Nov 21;6:e5988.  [Abstract]

    C6/36 cells are treated with 3-MA, Rapa or CQ for 36 h, 6 h and 36 h, respectively and then subjected to MDC staining. Mock and DMSO treated C6/36 cells are used as controls.

    Rapamycin purchased from MCE. Usage Cited in: PeerJ. 2018 Nov 21;6:e5988.  [Abstract]

    C6/36 cells are treated with 3-MA, Rapa or CQ for 36 h, 6 h and 36 h, respectively. For Rapa plus CQ treatment, C6/36 cells are treated with CQ for 30 h then treated with Rapa for 6 h. Mock and DMSO treated C6/36 cells are used as controls. After the treatment, the levels of AaAtg8-I and AaAtg8-II are analysed by immunoblotting using antibody against AaAtg8.

    Rapamycin purchased from MCE. Usage Cited in: Int J Ophthalmol. 2018 May 18;11(5):712-718.  [Abstract]

    Western blotting shows that Rapamycin treatment downregulates p-mTOR protein levels in infected and uninfected corneal tissues compared to the vehicle group.

    Rapamycin purchased from MCE. Usage Cited in: Evid Based Complement Alternat Med. 2018 Jun 26;2018:6049498.  [Abstract]

    Western blot analysis of AKT, p-Akt, mTOR, p-mTOR, FOXO1 and p-FOXO1 expression in U-87 MG cells after treatment with LY294002 (20 μM), Rapamycin (50 nM) or NAC (5 mM) with or without Xihuang pill (XHP).

    Rapamycin purchased from MCE. Usage Cited in: Cell Physiol Biochem. 2018;48(6):2318-2336.  [Abstract]

    Cells are pretreated with 5 mM 3-MA or 2 μM for 1 h and then exposed to 40 μM EPA and 10 μM Rp for 48 h. Cell extracts are prepared and subjected to western blot analysis.

    Rapamycin purchased from MCE. Usage Cited in: Cell Physiol Biochem. 2018;48(6):2318-2336.  [Abstract]

    Cells are treated with Rapamycin (Rp; 10 μM)+Eicosapentaenoic acid (EPA; 40 μM) with or without Chloroquine (CQ; 5 μM) for 48 h. Cell extracts are prepared and subjected to western blot analysis.

    Rapamycin purchased from MCE. Usage Cited in: Nat Commun. 2017 Jun 8;8:15617.  [Abstract]

    Immunoblot analysis of KRAS protein levels in parental (P) and resistant derivatives (R1 and R2) following 4 h treatment with the corresponding inhibitors Rapamycin, AZD2014, MLN0128, BEZ235 and 4EGI-1. Images are cropped for clarity from the same exposure of the same membrane.

    Rapamycin purchased from MCE. Usage Cited in: J Clin Invest. 2017 Sep 1;127(9):3339-3352.  [Abstract]

    Phosphorylation of SMAD1/5/8 and SMAD2/3 in FOP-iMSCs. Serum-starved FOP-iMSCs are pretreated with 10 nM Rapamycin (Rapa), 1 μM DMH1, or 1 μM SB-431542 for 1 hour.

    Rapamycin purchased from MCE. Usage Cited in: PLoS One. 2017 Nov 29;12(11):e0188748.  [Abstract]

    FTY720 reverses activation of autophagy induced by mTOR inhibitor, rapamycin. The impact of FTY720 and Rapamycin on the expression of Beclin1 and LC3 is evaluated by western blotting. Results are representative of 4 independent experiments.

    Rapamycin purchased from MCE. Usage Cited in: PLoS One. 2017 Jun 21;12(6):e0179772.  [Abstract]

    RAW264.7 cells transfected with miR-144-3p control or miR-144-3p mimic in full medium with or without 50μg/mL Rapamycin or 0.1% DMSO. 50 μg of total cell extracts are analyzed by Western blotting with a mouse anti-SQSTM1/p62 antibody. The p62 levels are detected by Western-blot (upper). Quantitative analysis of the p62 band normalized to β-actin is shown (lower).

    Rapamycin purchased from MCE. Usage Cited in: Biochem Pharmacol. 2016 Dec 15;122:42-61.  [Abstract]

    Inhibition of SREBPs processing by AHI is dependent on LKB-1/AMPK/mTOR pathway. (A) HepG2 cells are incubated with or without MHY1485 or Rapamycin for 1 h, the cells are switched to medium D in the presence of vehicle, or AHI. (B) HepG2 cells are incubated with or without Compound C for 1 h, the cells are switched to medium D in the presence of vehicle, or AHI.

    Rapamycin purchased from MCE. Usage Cited in: Sci Bull. 2015 Dec;60(24):2120-2128.

    CNE-2Z cells are treated with AZD8055 or Rapamycin with or without 1 T SMF for 3 d before they are harvested for Western blot.
    • 生物活性

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Rapamycin (Sirolimus; AY 22989) is a potent and specific mTOR inhibitor with an IC50 of 0.1 nM in HEK293 cells. Rapamycin binds to FKBP12 and specifically acts as an allosteric inhibitor of mTORC1[1]. Rapamycin is an autophagy activator, an immunosuppressant[2].

    IC50 & Target[1][2]

    mTOR

    0.1 nM (IC50, in HEK293 cells )

    Microbial Metabolite

     

    Autophagy

     

    Human Endogenous Metabolite

     

    体外研究
    (In Vitro)

    Rapamycin(12.5-100 nM;24 小时)处理在所有测试的细胞系(A549、SPC-A-1、95D 和 NCI-H446 细胞)中以剂量依赖性方式对肺癌细胞增殖产生适度抑制作用,达到约 100 nM 时细胞增殖减少 30-40%,而 12.5 nM 时减少约 10%[3]
    将肺癌细胞系 95D 细胞单独或联合暴露于 Rapamycin(10 nM、20 nM)和 RP-56976(1 nM、10 nM)(Rapamycin 20 nM + RP-56976 10 nM)。单独暴露于 Rapamycin 或 RP-56976 24 小时后,不会显着改变 ERK1/2 的表达或磷酸化水平,而 Rapamycin 与 RP-56976 联合处理的细胞表现出 ERK1/2 磷酸化水平的显着降低[3]

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Cell Viability Assay[3]

    Cell Line: Lung cancer cell lines A549, SPC-A-1, 95D and NCI-H446
    Concentration: 12.5 nM, 25 nM, 50 nM, 100 nM
    Incubation Time: 24 hours
    Result: Treatment exerted modest inhibitory effect on lung cancer cell proliferation in a dose-dependent manner in all cell lines.

    Western Blot Analysis[3]

    Cell Line: 95D cells
    Concentration: 10 nM and 20 nM
    Incubation Time: 24 hours
    Result: Combination treatment with RP-56976 decreased phosphorylation of ERK.
    体内研究
    (In Vivo)

    Rapamycin (2.0 mg/kg; 腹腔内注射; 每隔一天;28 天) 单独使用有中等的抑制作用。然而,与对照组、Rapamycin 组相比,二甲双胍联合 Rapamycin 对肿瘤生长的抑制作用明显增强[4]

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Model: 24 male nu/nu mice aged 4-5 week old (15-20 g)[4]
    Dosage: 2.0 mg/kg
    Administration: Intraperitoneal injection; every other day; 28 days
    Result: Had a moderate inhibitory effect in monotherapy group. The combination with Metformin exerted a significantly increased inhibition of tumor growth.
    Clinical Trial
    分子量

    914.17

    Formula

    C51H79NO13

    CAS 号
    性状

    固体

    颜色

    White to off-white

    中文名称

    雷帕霉素;西罗莫司

    结构分类
    初始来源

    bacterium Streptomyces hygroscopicus

    运输条件

    Room temperature in continental US; may vary elsewhere.

    储存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    溶解性数据
    In Vitro: 

    DMSO 中的溶解度 : 125 mg/mL (136.74 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

    Ethanol 中的溶解度 : 50 mg/mL (54.69 mM; 超声助溶)

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 1.0939 mL 5.4694 mL 10.9389 mL
    5 mM 0.2188 mL 1.0939 mL 2.1878 mL
    查看完整储备液配制表

    * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
    储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

    • 摩尔计算器

    • 稀释计算器

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    质量
    =
    浓度
    ×
    体积
    ×
    分子量 *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    浓度 (start)

    C1

    ×
    体积 (start)

    V1

    =
    浓度 (final)

    C2

    ×
    体积 (final)

    V2

    In Vivo:

    请根据您的 实验动物和给药方式 选择适当的溶解方案。

    以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:
    ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用
    以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

    • 方案 一

      请依序添加每种溶剂: 10% EtOH    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (2.73 mM); 悬浊液

      此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的均匀悬浊液,悬浊液可用于口服和腹腔注射。

      1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 EtOH 储备液加到 400 μL PEG300 中,混合均匀;再向上述体系中加入 50 μL Tween-80,混合均匀;然后再继续加入 450 μL 生理盐水 定容至 1 mL

      生理盐水的配制:将 0.9 g 氯化钠,溶解于 ddH₂O 并定容至 100 mL,可以得到澄清透明的生理盐水溶液。
    • 方案 二

      请依序添加每种溶剂: 10% EtOH    90% (20% SBE-β-CD in Saline)

      Solubility: 2.5 mg/mL (2.73 mM); 悬浊液; 超声助溶

      此方案可获得 2.5 mg/mL的均匀悬浊液,悬浊液可用于口服和腹腔注射。

      1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 EtOH 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中,混合均匀。

      20% SBE-β-CD in Saline 的配制(4°C,储存一周):2 g SBE-β-CD(磺丁基醚 β-环糊精)粉末定容于 10 mL 的生理盐水中,完全溶解至澄清透明。
    动物溶解方案计算器
    请输入动物实验的基本信息:

    给药剂量

    mg/kg

    动物的平均体重

    g

    每只动物的给药体积

    μL

    动物数量

    由于实验过程有损耗,建议您多配一只动物的量
    请输入您的动物体内配方组成:
    %
    DMSO +
    +
    %
    Tween-80 +
    %
    Saline
    如果您的动物是免疫缺陷鼠或者体弱鼠,建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
    方案所需 助溶剂 包括:DMSO ,均可在 MCE 网站选购。 Tween 80,均可在 MCE 网站选购。
    计算结果
    工作液所需浓度 : mg/mL
    储备液配制方法 : mg 药物溶于 μL  DMSO(母液浓度为 mg/mL)。
    您所需的储备液浓度超过该产品的实测溶解度,以下方案仅供参考,如有需要,请与 MCE 中国技术支持联系。
    动物实验体内工作液的配制方法 : 取 μL DMSO 储备液,加入 μL  μL ,混合均匀至澄清,再加 μL Tween 80,混合均匀至澄清,再加 μL 生理盐水
    连续给药周期超过半月以上,请谨慎选择该方案。
    请确保第一步储备液溶解至澄清状态,从左到右依次添加助溶剂。您可采用超声加热 (超声清洗仪,建议频次 20-40 kHz),涡旋吹打等方式辅助溶解。
    纯度 & 产品资料

    纯度: 99.94%

    参考文献

    完整储备液配制表

    * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
    储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    Ethanol / DMSO 1 mM 1.0939 mL 5.4694 mL 10.9389 mL 27.3472 mL
    5 mM 0.2188 mL 1.0939 mL 2.1878 mL 5.4694 mL
    10 mM 0.1094 mL 0.5469 mL 1.0939 mL 2.7347 mL
    15 mM 0.0729 mL 0.3646 mL 0.7293 mL 1.8231 mL
    20 mM 0.0547 mL 0.2735 mL 0.5469 mL 1.3674 mL
    25 mM 0.0438 mL 0.2188 mL 0.4376 mL 1.0939 mL
    30 mM 0.0365 mL 0.1823 mL 0.3646 mL 0.9116 mL
    40 mM 0.0273 mL 0.1367 mL 0.2735 mL 0.6837 mL
    50 mM 0.0219 mL 0.1094 mL 0.2188 mL 0.5469 mL
    DMSO 60 mM 0.0182 mL 0.0912 mL 0.1823 mL 0.4558 mL
    80 mM 0.0137 mL 0.0684 mL 0.1367 mL 0.3418 mL
    100 mM 0.0109 mL 0.0547 mL 0.1094 mL 0.2735 mL
    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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