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  • 雷帕霉素|T1537

雷帕霉素|T1537

Rapamycin
53123-88-9
133 1mg 起订
283 5mg 起订
455 10mg 起订
上海 更新日期:2026-01-06

TargetMol中国(陶术生物)

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产品详情:

中文名称:
雷帕霉素
英文名称:
Rapamycin
CAS号:
53123-88-9
品牌:
TargetMol
产地:
美国
保存条件:
keep away from moisture,store at low temperature,keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
纯度规格:
99.90%
产品类别:
抑制剂
货号:
T1537

Product Introduction

Bioactivity

名称Rapamycin
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.
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].
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].
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].
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]
存储条件keep away from moisture,store at low temperature,keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
溶解度Ethanol : 100 mg/mL (109.39 mM), Sonication is recommended.
H2O : Insoluble
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 10 mg/mL (10.94 mM), Solution.
DMSO : 257.5 mg/mL (281.68 mM), Sonication is recommended.
关键字Rapamycin | NSC2260804 | NSC 2260804 | mTORC1 | mTOR | Mammalian target of Rapamycin | Inhibitor | inhibit | immunosuppressant | HEK293 | Fungal | FKBP12 | FKBP | FK506-binding protein | EndogenousMetabolite | Endogenous Metabolite | Bacterial | AY-22989 | AY22989 | Autophagy | Antibiotic
相关产品Glycerol | Aceglutamide | Calcium Propionate | Benzyl propionate | Sucrose | Neomycin sulfate | BES | Dimethyl sulfoxide | Gluconate Calcium | Thymidine | Sodium diacetate | D(+)-Raffinose pentahydrate
相关库抑制剂库 | 抗癌上市药物库 | 经典已知活性库 | 抗真菌库 | 已知活性化合物库 | 抗衰老化合物库 | 抗癌天然产物库 | 抗病毒库 | FDA 上市药物库 | FDA 上市激酶抑制剂库 | 抗癌药物库 | 抗感染天然产物库
br
西罗莫司|||雷帕霉素|||Sirolimus|||NSC-2260804|||AY 22989|TargetMol

公司简介

上海陶术生物科技有限公司为美国Target Molecule Corp. ( Target Mol ) 在上海建立的全资子公司。我们与美国波士顿、德国慕尼黑的同事一起,为北美、欧洲和亚洲从事药物研发和生物学研究的科学家提供优质的产品和专业的服务。公司下设筛选事业部,化学事业部,生物事业部和新材料部。 从虚拟筛选到实体化合物分子供应;从商业化产品销售到个性化定制合成;从对明确靶点的分子筛选到对明确分子的多靶点筛选,从高通量筛选到化学结构优化,我们都可以满足您的科研用品及技术服务的需求。 经过在中国市场五年的精心耕耘,我们已成为筛选化合物领域优秀的供应商,为超过五百家学校和各类企业提供了品质卓越的小分子化合物和药物筛

成立日期 (13年)
注册资本 566.2651万人民币
员工人数 100-500人
年营业额 ¥ 1亿以上
经营模式 贸易,试剂,定制,服务
主营行业 化学试剂,生物活性小分子

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