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Merck
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重要文件

R0395

Sigma-Aldrich

Rapamycin

from Streptomyces hygroscopicus, ≥95% (HPLC), powder, mTOR inhibitor

同義詞:

AY 22989, 西罗莫司, 雷帕霉素

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About This Item

經驗公式(希爾表示法):
C51H79NO13
CAS號碼:
分子量::
914.17
MDL號碼:
分類程式碼代碼:
12352200
PubChem物質ID:
NACRES:
NA.77

產品名稱

Rapamycin 来源于吸水链霉菌, ≥95% (HPLC), powder

品質等級

化驗

≥95% (HPLC)

形狀

powder

顏色

off-white

溶解度

ethanol: 2 mM
DMSO: soluble

抗生素活性譜

fungi
yeast

作用方式

enzyme | inhibits
protein synthesis | interferes

儲存溫度

−20°C

SMILES 字串

CO[C@@H]1C[C@@H](CC[C@H]1O)C[C@@H](C)[C@@H]2CC(=O)[C@H](C)\C=C(C)\[C@@H](O)[C@@H](OC)C(=O)[C@H](C)C[C@H](C)\C=C\C=C\C=C(C)\[C@H](C[C@@H]3CC[C@@H](C)[C@@](O)(O3)C(=O)C(=O)N4CCCC[C@H]4C(=O)O2)OC

InChI

1S/C51H79NO13/c1-30-16-12-11-13-17-31(2)42(61-8)28-38-21-19-36(7)51(60,65-38)48(57)49(58)52-23-15-14-18-39(52)50(59)64-43(33(4)26-37-20-22-40(53)44(27-37)62-9)29-41(54)32(3)25-35(6)46(56)47(63-10)45(55)34(5)24-30/h11-13,16-17,25,30,32-34,36-40,42-44,46-47,53,56,60H,14-15,18-24,26-29H2,1-10H3/b13-11+,16-12+,31-17+,35-25+/t30-,32-,33-,34-,36-,37+,38+,39+,40-,42+,43+,44-,46-,47+,51-/m1/s1

InChI 密鑰

QFJCIRLUMZQUOT-HPLJOQBZSA-N

基因資訊

human ... FKBP1A(2280)

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一般說明

化学结构:大环内酯
雷帕霉素来源于吸湿链霉菌。它可以抑制病毒复制。这种天然抗真菌抗生素是一种经过验证的抗衰老剂。雷帕霉素能够显著抑制mTORC1且不受年龄的影响。它能够抑制蛋白激酶C活性,增强A6细胞的离子转运。它还能抑制膜和细胞质制剂中的免疫反应。此外,它对内源性mRNA的翻译具有特异性作用,并通过阻断信号通路中p70s6k的激活来抑制5′TOP mRNA的翻译。雷帕霉素具有抗肿瘤特性。

應用

来自吸湿链霉菌的雷帕霉素已用于:
  • 处理BV2细胞或BV2- lc3细胞,进行自噬实验
  • 作为自噬激活剂,用于转染FOXO3小干扰RNA慢病毒载体(siFOXO3)的骨髓间充质干细胞(BM-MSCs),以研究Forkhead Box O3(FOXO3)对BM-MSC
  • 自噬的影响,以预孵育绒毛并抑制雷帕霉素复合物1 (mTORC1)信号传导的哺乳动物靶点

生化/生理作用

一种与雷帕霉素(mTOR)分子靶点结合并抑制其作用的大环三烯抗生素。 它与FKBP12形成复合物,结合并抑制雷帕霉素(mTOR)的分子靶点。 雷帕霉素是一种有效的免疫抑制剂,并具有抗癌活性。

特點和優勢

《受体分类和信号转导》手册的 PKB/Akt 页面有该化合物的介绍。想要浏览手册的其他页面, 请单击此处

其他說明

保持容器密封,存放在干燥,通风良好的地方。保持干燥

象形圖

Health hazard

訊號詞

Warning

危險聲明

危險分類

Carc. 2 - Repr. 2

儲存類別代碼

11 - Combustible Solids

水污染物質分類(WGK)

WGK 2

個人防護裝備

Eyeshields, Gloves, type N95 (US)


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存取文件庫

Line Heylen et al.
Clinical infectious diseases : an official publication of the Infectious Diseases Society of America, 60(10), 1505-1511 (2015-02-15)
Transplant recipients are at risk for invasive aspergillosis (IA), associated with a significant mortality rate. Renal transplant-specific risk factors have not been established. Forty-one adult kidney transplant recipients diagnosed with proven or probable IA from 1995 through 2013 were identified
Marlous J Groenewoud et al.
Open biology, 3(12), 130185-130185 (2013-12-20)
Mitochondrial dysfunction has been associated with various diseases, such as cancer, myopathies, neurodegeneration and obesity. Mitochondrial homoeostasis is achieved by mechanisms that adapt the number of mitochondria to that required for energy production and for the supply of metabolic intermediates
Stephanie James et al.
The American journal of tropical medicine and hygiene, 90(1), 6-10 (2013-11-28)
As global efforts to eliminate malaria intensify, accurate information on vector populations and transmission dynamics is critical for directing control efforts, developing new control tools, and predicting the effects of these interventions under various conditions. Currently available sampling tools for
A V Tinker et al.
Gynecologic oncology, 130(2), 269-274 (2013-05-16)
HPV infection has been associated with deregulation of the PI3K-Akt-mTOR pathway in invasive cervical carcinomas. This 2-stage phase II study assessed the activity of the mTOR inhibitor, temsirolimus, in patients with measurable metastatic and/or locally advanced, recurrent carcinoma of the
Benjamin Albert et al.
The Journal of cell biology, 202(2), 201-210 (2013-07-24)
Chromosomes architecture is viewed as a key component of gene regulation, but principles of chromosomal folding remain elusive. Here we used high-throughput live cell microscopy to characterize the conformation and dynamics of the longest chromosome of Saccharomyces cerevisiae (XII). Chromosome

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