雷帕霉素|T1537

價(jià)格	￥133	￥283	￥455
包裝	1mg	5mg	10mg

最小起訂量	1mg
發(fā)貨地	上海
更新日期	2024-12-02

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產(chǎn)品詳情

中文名稱:雷帕霉素	英文名稱:Rapamycin
CAS:53123-88-9	品牌: TargetMol
產(chǎn)地: 美國	保存條件: Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
純度規(guī)格: 99.03%	產(chǎn)品類別: 抑制劑
貨號(hào): T1537

Product Introduction

Bioactivity

名稱	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.
細(xì)胞實(shí)驗(yàn)	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].
激酶實(shí)驗(yàn)	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].
動(dòng)物實(shí)驗(yàn)	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].
體外活性	方法：正常人腎上皮細(xì)胞 HRECs 用 Rapamycin (0.01-1000 nmol/L) 處理 6 天，使用 MTT 方法檢測(cè)細(xì)胞生長抑制情況。結(jié)果：Rapamycin 劑量依賴性地抑制 HRECs 細(xì)胞生長，在10 nmol/L 的濃度下，細(xì)胞活力降低了40%。[1] 方法：人宮頸癌細(xì)胞 HeLa 和人前列腺癌細(xì)胞 PC3 用 Rapamycin (100 nM) 處理 0.5-24 h，使用 Immunoprecipitation 方法檢測(cè)靶點(diǎn)蛋白表達(dá)水平。結(jié)果：Rapamycin 對(duì) mTOR、raptor 和 rictor 的表達(dá)水平影響不大，在 0.5 h 內(nèi)顯著降低了與 mTOR 結(jié)合的 raptor，在 24 h 時(shí)降低了與 mTOR 結(jié)合的 rictor。Rapamycin 長期處理細(xì)胞抑制 mTORC2 的組裝。[2] 方法：人血管內(nèi)皮細(xì)胞用 Rapamycin (1-100 ng/mL) 處理 48 h，使用 Wound-healing 方法檢測(cè)細(xì)胞遷移情況。結(jié)果：Rapamycin 劑量依賴性地抑制人血管內(nèi)皮細(xì)胞的遷移能力。[3]
體內(nèi)活性	方法：為研究 Rapamycin 壽命的影響，將 Rapamycin (8 mg/kg in DMSO+5% PEG-400+5% Tween-80) 腹腔注射給 20–21 個(gè)月大的 C57BL/6J 小鼠，每天一次，持續(xù)三個(gè)月。結(jié)果：Rapamycin 治療 3 個(gè)月足以將中年小鼠的預(yù)期壽命提高60%，并改善其健康壽命。[4] 方法：為確定 Rapamycin 治療癲癇的合適劑量，將 Rapamycin (0.1-3 mg/kg in 4% ethanol+5% Tween 80+5% PEG 400) 腹腔注射給 Sprague-Dawley 大鼠，每天一次，持續(xù)四周。結(jié)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 處理的大鼠沒有明顯的不良反應(yīng)，而用 1.0 和 3.0 mg/kg Rapamycin 處理的大鼠的身體、脾臟和胸腺重量顯著降低，表現(xiàn)出認(rèn)知障礙和焦慮。Rapamycin 劑量不能抑制 mTOR 治療癲癇而不引起任何副作用，但 1 mg/kg 可能是年輕大鼠抑制 mTOR 的最佳劑量，副作用相對(duì)較少。[5]
存儲(chǔ)條件	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
溶解度	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.
關(guān)鍵字	AY22989 \| Bacterial \| FK506-binding protein \| immunosuppressant \| mTORC1 \| mTOR \| Fungal \| Mammalian target of Rapamycin \| inhibit \| AY-22989 \| Autophagy \| Rapamycin \| Endogenous Metabolite \| Inhibitor \| Antibiotic \| NSC2260804 \| HEK293 \| FKBP12 \| FKBP \| NSC 2260804
相關(guān)產(chǎn)品	Guanidine hydrochloride \| Daidzein \| Glycerol \| Doxycycline \| Sucrose \| Neomycin sulfate \| Hydroxychloroquine \| Ferulic Acid \| 3-Indoleacetic acid \| Thymidine \| Sulfamethoxazole sodium \| Paeonol
相關(guān)庫	經(jīng)典已知活性庫 \| 已知活性化合物庫 \| 抗真菌庫 \| 抗衰老化合物庫 \| FDA 上市激酶抑制劑庫 \| 藥物功能重定位化合物庫 \| 高通量篩選天然產(chǎn)物庫 \| 抗癌藥物庫

關(guān)鍵字：西羅莫司|||雷帕霉素|||Sirolimus|||NSC-2260804|||AY 22989|TargetMol

公司簡(jiǎn)介

上海陶術(shù)生物科技有限公司為美國Target Molecule Corp. ( Target Mol ) 在上海建立的全資子公司。我們與美國波士頓、德國慕尼黑的同事一起，為北美、歐洲和亞洲從事藥物研發(fā)和生物學(xué)研究的科學(xué)家提供優(yōu)質(zhì)的產(chǎn)品和專業(yè)的服務(wù)。公司下設(shè)篩選事業(yè)部，化學(xué)事業(yè)部，生物事業(yè)部和新材料部。從虛擬篩選到實(shí)體化合物分子供應(yīng)；從商業(yè)化產(chǎn)品銷售到個(gè)性化定制合成；從對(duì)明確靶點(diǎn)的分子篩選到對(duì)明確分子的多靶點(diǎn)篩選，從高通量篩選到化學(xué)結(jié)構(gòu)優(yōu)化，我們都可以滿足您的科研用品及技術(shù)服務(wù)的需求。經(jīng)過在中國市場(chǎng)五年的精心耕耘，我們已成為篩選化合物領(lǐng)域優(yōu)秀的供應(yīng)商，為超過五百家學(xué)校和各類企業(yè)提供了品質(zhì)卓越的小分子化合物和藥物篩

成立日期	2013-04-18 （12年）	注冊(cè)資本	566.2651萬人民幣
員工人數(shù)	100-500人	年?duì)I業(yè)額	￥ 1億以上
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公司成立：12年
注冊(cè)資本：566.2651萬人民幣
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