1. Metabolic Enzyme/Protease Autophagy Apoptosis Anti-infection
  2. Proteasome Autophagy Mitophagy Apoptosis Endogenous Metabolite Antibiotic Bacterial
  3. Celastrol

Celastrol  (Synonyms: 雷公藤红素; Tripterine; Tripterin)

目录号: HY-13067 纯度: 99.68%
COA 产品使用指南

Celastrol (Tripterine) 是一种蛋白酶体抑制剂,有效且优先抑制 20S 蛋白酶体的胰凝乳蛋白酶样活性,IC50 为 2.5 μM。此外,Celastrol 也是一种对标准和临床 methicillin-resistant Staphylococcus aureus (MRSA) 菌株具有强大抗菌活性的抗生素 (antibiotic),通过与 P5CDH 结合诱导氧化应激并抑制 DNA 合成。

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Celastrol Chemical Structure

Celastrol Chemical Structure

CAS No. : 34157-83-0

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5 mg ¥523
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10 mg ¥837
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50 mg ¥2278
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100 mg ¥3255
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Customer Review

Other Forms of Celastrol:

MCE 顾客使用本产品发表的 35 篇科研文献

WB

    Celastrol purchased from MCE. Usage Cited in: Cell Death Dis. 2018 May 22;9(6):601.  [Abstract]

    Serum-starved HK-2 cells are pretreated with or without indicated concentrations of Celastrol (CEL) for 1 h and then stimulated with TGF-β1 (10 ng/mL) for 24 h. Representative western blots and quantification data of CB2R expression in HK-2 cells are presented.

    Celastrol purchased from MCE. Usage Cited in: Life Sci. 2018 Jul 15;205:136-144.  [Abstract]

    Effects of Celastrol (CEL) on the expression of F4/80 in plantar skin. CEL treatment suppresses macrophage expression in plantar skin. Western blot assay shows significantly downregulated F4/80 levels in 10 and 20 μg/paw CEL groups.

    Celastrol purchased from MCE. Usage Cited in: RSC Adv. 2016,6, 42537-42544.

    Celastrol is able to increase HSP70 protein expression by more than 1.8-fold in PC-3 cells after 24 h of incubation.

    Celastrol purchased from MCE. Usage Cited in: Mol Biosyst. 2016 Dec 20;13(1):83-91.  [Abstract]

    Validation of selected targets of Celastrol identified by competitive proteomics. Western blotting (by using anti-GSTO1 and anti-PDI antibodies) of the pull-down samples upon labeling with IA-yne.
    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Celastrol (Tripterine;Tripterin) is a proteasome inhibitor which potently and preferentially inhibits the chymotrypsin-like activity of a purified 20S proteasome with IC50 of 2.5 μM. In addition, Celastrol is also an antibiotic with potent antimicrobial activity against standard and clinical methicillin-resistant Staphylococcus aureus (MRSA) strains, inducing oxidative stress and inhibiting DNA synthesis by binding to P5CDH[1][2][3].

    IC50 & Target

    Human Endogenous Metabolite

     

    体外研究
    (In Vitro)

    Celastrol (Tripterine;Tripterin) 以浓度依赖性方式显著抑制 PC-3 细胞中蛋白酶体胰凝乳蛋白酶的活性;在 2.5 μM 时,它达到约 55% 的抑制,与其对纯化的 20S 蛋白酶体的效力相当 (IC50=2.5 μM)。此外,观察到 IκB-α、Bax 和 p27 水平升高,这是用 Celastrol 处理的 PC-3 细胞中蛋白酶体的三种众所周知的靶蛋白[1]

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

    体内研究
    (In Vivo)

    用 Celastrol (1-3 mg/kg/d,腹腔注射,1-31 天) 处理携带 PC-3 肿瘤的裸鼠导致显著抑制肿瘤生长 (65-93%)[1]
    用 3 和 6 mg/kg Celastrol 处理后,丙二醛 (MDA) 水平分别显著降低 35.2% 和 36.7% (P<0.05)。用 3 和 6 mg/kg 的 Celastrol 处理可显著将 GSH 水平 (P<0.05) 恢复到几乎正常的水平[2]

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

    Clinical Trial
    分子量

    450.61

    Formula

    C29H38O4

    CAS 号
    性状

    固体

    颜色

    Orange to reddish brown

    中文名称

    雷公藤红素;南蛇藤素;南蛇藤醇;苦瓜甙;苦瓜苷;苦瓜素;苦瓜皂甙

    结构分类
    初始来源
    运输条件

    Room temperature in continental US; may vary elsewhere.

    储存方式
    Powder -20°C 3 years
    In solvent -80°C 6 months
    -20°C 1 month
    溶解性数据
    细胞实验: 

    DMSO 中的溶解度 : 33.33 mg/mL (73.97 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)

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 2.2192 mL 11.0961 mL 22.1921 mL
    5 mM 0.4438 mL 2.2192 mL 4.4384 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

    动物实验:

    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% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (5.55 mM); 澄清溶液

      此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液。

      1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 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。
    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: 99.90%

    参考文献
    Kinase Assay
    [1]

    A purified rabbit 20S proteasome (0.1 μg) is incubated with 40 μM of various fluorogenic peptide substrates in 100 μL assay buffer (20 mM Tris-HCl ,pH 7.5), in the presence of Celastrol or Oridonin at different concentrations or in the solvent DMSO for 2 hours at 37°C, followed by measurement of inhibition of each proteasomal activity[1].

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

    Cell Assay
    [1]

    Prostate cancer cells (5,000-8,000) are plated in each well of a 96-well plate and then treated with either DMSO, Celastrol, or Oridonin at different concentrations for 12 to 16 hours, followed by an additional 2-hour incubation with Z-Gly-Gly-Leu-AMC (at 40 μM). After that, the proteasome activity is measured using the whole plate[1].

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

    Animal Administration
    [1][2]

    Mice[1]
    Male nude immunodeficient mice NCRNU-M, aged 5 weeks, are used. On day 0, human prostate cancer PC-3 or C4-2B cells (5-10×106) suspended in 0.1 mL of serum-free RPMI 1640 are inoculated s.c. in the right flank of each mouse (four mice per group). For the first experiment using PC-3 cells, on day 14 after inoculation, the animals started daily i.p. injection with either 50 to 100 μL of a vehicle [10% DMSO, 70% Cremophor/ethanol (3:1), and 20% PBS], and 1.0 or 3.0 mg/kg of Celastrol. Tumor sizes are measured daily using calipers and their volumes are calculated using a standard formula: width2×length/2. Body weight is measured weekly. To study whether the proteasome is inhibited in an early phase of the experiment, after 3 days of treatment, one control and one 3.0 mg/kg Celastrol -treated mouse is sacrificed. The rest are sacrificed after 16 days of treatment when control tumors reach 1,400 mm3. For the second PC-3 tumor experiment, 12 days after inoculation, mice are randomly divided into three groups and treated with either control, Celastrol, or Oridonin at 1.5 mg/kg daily for the duration of the study (31 days). In another experiment, to study the effects of Celastrol on AR expression, nude mice bearing C4-2B tumors receive daily i.p. injection of the vehicle or 3.0 mg/kg Celastrol.
    Rats[2]
    Male Sprague-Dawley (SD) rats (n=90, 6 weeks old), weighing 161±9 g, are randomly divided into the control (NC) and the high energy diet (HED) groups. In the control group, the animals receive a standard chow diet, while the rats in the HED group are fed with an additional high energy emulsion. After 8 weeks on their respective diets, Streptozotocin (STZ; 45 mg/kg) dissolved in 0.1 mol/l citrate buffer (pH 4.5) is injected into the caudal vein of the rats in the HED group to establish a model of T2DM, while the rats in the control group are injected with sodium citrate buffer. The rats with blood glucose levels ≥16.7 mM at 7 days after the STZ injection are selected as the model of diabetes. On average, 80% of the rats injected with STZ met these criteria. At 1 week following the injection of STZ, the rats with successfully-induced diabetes are randomly divided into the diabetes model (DM) group, the Celastrol low-dose group (1 mg/kg/day), the Celastrol middle-dose group (3 mg/kg/day) and the Celastrol high-dose group (6 mg/kg/day) (n=15 rats per group). The rats in the treatment groups are administered Celastrol by gavage, whereas the rats in the NC and DM groups are administered an equal amount of distilled water (2 mL). Following 8 weeks of the respective treatments, rats are anesthetized with an intraperitoneal injection of sodium pentobarbital (30 mg/kg body weight) and tissue samples are collected for analysis. The paravertebral muscle is excised from the rat bodies, and is cut perpendicularly along the longitudinal axis and fixed in phosphate-buffered 20% formaldehyde. Histological paraffin-embedded sections (5 μm) are then prepared for H&E staining. The sections of paravertebral muscle are snap-frozen in liquid nitrogen and stored at ?80°C until further analysis.

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

    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
    DMSO 1 mM 2.2192 mL 11.0961 mL 22.1921 mL 55.4804 mL
    5 mM 0.4438 mL 2.2192 mL 4.4384 mL 11.0961 mL
    10 mM 0.2219 mL 1.1096 mL 2.2192 mL 5.5480 mL
    15 mM 0.1479 mL 0.7397 mL 1.4795 mL 3.6987 mL
    20 mM 0.1110 mL 0.5548 mL 1.1096 mL 2.7740 mL
    25 mM 0.0888 mL 0.4438 mL 0.8877 mL 2.2192 mL
    30 mM 0.0740 mL 0.3699 mL 0.7397 mL 1.8493 mL
    40 mM 0.0555 mL 0.2774 mL 0.5548 mL 1.3870 mL
    50 mM 0.0444 mL 0.2219 mL 0.4438 mL 1.1096 mL
    60 mM 0.0370 mL 0.1849 mL 0.3699 mL 0.9247 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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    目录号:
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