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Rapamycin雷帕霉素

Rapamycin雷帕霉素

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Rapamycin雷帕霉素用途及描述:科研试剂,广泛应用于分子生物学,药理学等科研方面。雷帕霉素(西罗莫司)是目前世界上Z新的强效免疫抑制剂。

Rapamycin雷帕霉素的详细资料:



Rapamycin雷帕霉素参数

Rapamycin (Sirolimus) 雷帕霉素(西罗莫司)

别  名

西罗莫司(sirolimus)

 

 

Cas 号

53123-88-9

分子式

C51H79NO13  

分子量

914.18

结构式

 

 

Rapamycin雷帕霉素定义:

一种新型大环内酯类免疫抑制药物。通过与相应免疫嗜素RMBP结合抑制细胞周期G0期和G1期,阻断G1进入S期而发挥作用,其效应为:①抑制T和B细胞增殖;②抑制IL-1、IL-2、IL-6和IFN-γ诱导的淋巴细胞增殖;③抑制IgG和供者特异性抗体(细胞毒抗体)产生;④抑制单核细胞增殖。可用于抗移植排斥反应和治疗类风湿性关节炎、红斑狼疮等自身免疫病。

溶解性:可溶解于DMSO (50mg/ml)、甲醇(50 mg/ml)、乙醇、丙酮、等有机溶剂;几乎不溶于水。

作用

本品抑制由抗原和细胞因子(白介素IL-2、IL-4和IL-15)激发的T淋巴细胞的活化和增殖,它亦抑制抗体的产生。在细胞中,西罗莫司与免疫嗜素,即FK结合蛋白-12(FKBP-12)结合,生成FKBP-12免疫抑制复合物。此复合物与哺乳动物的西罗莫司BA分子(mTOR,一种关键的调节激酶)结合并抑制其活性,从而抑制细胞周期中G1期向S期的发展。

Trusted Worldwide: more than 10,000 vials of our rapamycin have been shipped to more than 2,500 laboratories worldwide since 2002.

Immunosuppressant, related to FK-506, but without calcineurin inhibitory activity even when complexed to FK-506 binding protein. Selectively blocks signaling that leads to p70 S6 kinase activation (IC50 = 50 pM). Terada, N., et al. "Failure of rapamycin to block proliferation once resting cells have entered the cell cycle despite inactivation of p70 S6 kinase." J. Biol. Chem. 268: 12062-12068 (1993). Fingar, D.C., et al. "Dissociation of pp70 ribosomal protein S6 kinase from insulin-stimulated glucose transport in 3T3-L1 adipocytes." J. Biol. Chem. 268: 3005-3008 (1993). Price, D.J., et al. "Rapamycin-induced inhibition of the 70-kilodalton S6 protein kinase." Science 257: 973-977 (1992). Chung, J., et al. "Rapamycin-FKBP specifically blocks growth-dependent activation of and signaling by the 70 kd S6 protein kinases." Cell 69: 1227-1236 (1992).

Lymphokine-induced cell proliferation at the G1 phase is inhibited and apoptosis in a murine B cell line is induced by rapamycin. Rapamycin arrests the Saccharomyces cerevisiae cell cycle irreversibly in the G1 phase. Morice, W.G. ,et al. "Rapamycin-induced inhibition of p34cdc2 kinase activation is associated with G1/S-phase growth arrest in T lymphocytes." J. Biol. Chem. 268: 3734-3738 (1993). Kay, J.E., et al. "Inhibition of T and B lymphocyte proliferation by rapamycin." Immunology 72: 544-549 (1991). Heitman, J., et al. "Targets for cell cycle arrest by the immunosuppressant rapamycin in yeast." Science 253: 905-909 (1991).

Rapamycin extended n and maximal lifespan of both male and female mice when fed late in life. Harrison, D.E., et al. "Rapamycin fed late in life extends lifespan in genetically heterogeneous mice." Nature 460: 392-395 (2009).

Rapamycin has shown activity in slowing cellular and organismal aging. Rapamycin abolished nuclear blebbing, delayed the start of cellular senescence, and improved the degradation of progerin in Hutchinson-Gilford progeria syndrome fibroblast cells. It also reduced the ion of insoluble progerin aggregates and resulted in clearance through autophagic mechanisms in normal fibroblasts. Cao, K., et al. "Rapamycin reverses cellular phenotypes and enhances mutant protein clearance in Hutchinson-Gilford progeria syndrome cells." Sci. Transl. Med. 3: 89ra58 (2011).

Due to a different mechanism of action than FK506 and other immunosuppressants, rapamycin may prove to be important in organ transplant patient therapy. Fewer side effects than the standard anti-rejection treatments have been observed. Proliferation of activated T cells, but not apoptosis, is blocked by rapamycin. The induction of apoptosis of rejection-causing T cells reduces the tendency towards transplant rejection. Schwarz, C. and Oberbauer, R. "The future role of target of rapamycin inhibitors in renal transplantation." Curr Opin Urol. 12: 109-113 (2002). Wells, A.D. et al. "Requirement for T-cell apoptosis in the induction of peripheral transplantation tolerance." Nat. Med. 5: 1303-1307 (1999). Li, Y., et al. "Blocking both signal 1 and signal 2 of T-cell activation prevents apoptosis of alloreactive T cells and induction of peripheral allograft tolerance." Nat. Med. 5: 1298-1302 (1999).

We have had one lot of Selleck Chemical's rapamycin analyzed by a highly experienced and expert clinical analytical laboratory that specializes in rapamycin analyses. Using liquid chromatography - mass spectrometry, they found a purity of 96.7% (cis plus trans) for a lot of Selleck's rapamycin. In contrast, we have proven our rapamycin to be greater than 99% in purity for every lot, no exceptions.

More on the subject of rapamycin purity: HPLC analysis of rapamycin is somewhat complicated. Rapamycin forms several chromatographically separable species in solution, consisting perhaps of different conformers, tautomers, hydrates and/or isomers, but they are all in equilibrium with the major form, trans-rapamycin. We have shown this by collecting the individual impurity peaks in our rapamycin product and individually re-injecting them into the HPLC. In each case, upon re-injection the collected impurity peak is reduced or absent, and the major peak is again trans-rapamycin, of ~95% purity or higher, thus confirming re-equilibration back to the major trans-isomer of rapamycin. Because we find that all significant impurities (generally, those above 0.1%) in our product, including the cis-isomer, are in equilibrium with the trans isomer in the solution used for analysis, the actual purity of our product is >99% rapamycin, in all of its equilibrium forms. In contrast, material from other suppliers typically contains impurities that do not equilibrate with trans-rapamycin, and thus are genuine contaminants. These results also indicate that it is probably not possible to obtain the trans isomer in pure form, because in solution it will quickly re-equilibrate to the mixture of cis and trans.

储存条件:-20℃,避光防潮密闭干燥。

 

订购信息:

品名

产地

货号

规格

单价

备注

Rapamycin (Sirolimus) 雷帕霉素(西罗莫司)

MKbio

MZ0201-10MG

10MG

248

现货

Rapamycin (Sirolimus) 雷帕霉素(西罗莫司)

MKbio

MZ0201-100MG

100MG

680

现货

上海懋康生物科技有限公司是一家涉足于生命科学和生物技术域研究的试剂、仪器和实验室消耗品与实验服务工作,主要从事细胞生物学、植物学、分子生物学、免疫学、生物化学、蛋白组学。生物制药与诊断试剂研发生产等域。 本公司秉承“以人为本,以诚为信、合同守信”的经营理念。坚持"品质保障"的原则为广大客户提供优质产品。
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500ml

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500ml

1640培养基 1640 Medium

GIBCO

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10X1L

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10X1L

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12100-046

10X1L

DMEM(低糖)DMEM(Low Glucose)

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31600-034

10X1L

MEM 培养基

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41500-034

10X1L

M199培养基 M199 Medium

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31100-035

10X1L

F12培养基

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21700-075

10X1L

DMEM/F12培养基

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12400-024

10X1L

IMDM培养基

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10X1L

DMEM(高糖)培养液

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SH30022.01B

500ml

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500ml

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500ml

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SH30265.01B

500ml

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500ml

胰蛋白酶/EDTA消化液

Hyclone

SV30042.01

100ml

青/链霉素浓缩液

Hyclone

SV30010

100ml

Lipofectamine® 2000 Transfection Reagent
 脂质体2000

GIBCO

11668-027

0.75ml

Lipofectamine® 2000 Transfection Reagent
 脂质体2000

GIBCO

11668-019

1.5ml

B-27® Serum-Free Supplement (50X), Liquid 
 

GIBCO

17504-044

10ml

N-2 Supplement (100X), Liquid
 

GIBCO

17502-048

5ml

G-5 Supplement (100X), Liquid 

GIBCO

17503-012

1ml

SUPERSCRIPT II

invitrogen

18064014

 

SUPERSCRIPT III

invitrogen

18080044

 

SUPERSCRIPT III 1ST

invitrogen

18080051

 

Wizard® SV Gel and PCR Clean-Up System

promega

A9281

50 preps

Wizard® SV Gel and PCR Clean-Up System

promega

A9282

250 preps

Wizard® SV Gel and PCR Clean-Up System

promega

A9285

1000 preps

Dual-Glo™ Luciferase Assay System

promega

E2920

10ml

Dual-Glo™ Luciferase Assay System

promega

E2940

100ml

Dual-Glo™ Luciferase Assay System

promega

E2980

10 × 100ml

Dual-Luciferase® Reporter Assay System

promega

E1910

100 assays

Dual-Luciferase® Reporter Assay System 10-Pack

promega

E1960

1,000 assays

Dual-Luciferase® Reporter 1000 Assay System

promega

E1980

1,000 assays

ImProm-II™ Reverse Transcriptase

promega

A3803

500 reactions

ImProm-II™ Reverse Transcription System

promega

A3800

100 reactions

Reverse Transcription System

promega

A3500

100 reactions

CellTiter 96® Non-Radioactive Cell Proliferation Assay

promega

G4000

1,000 assays

CellTiter 96® Non-Radioactive Cell Proliferation Assay

promega

G4100

5,000 assays

CellTiter 96® AQueous One Solution Cell Proliferation Assay

promega

G3580

1,000 assays

CellTiter 96® AQueous One Solution Cell Proliferation Assay

promega

G3581

5,000 assays

CellTiter 96® AQueous One Solution Cell Proliferation Assay

promega

G3582

200 assays

CellTiter 96® AQueous Non-Radioactive Cell Proliferation Assay

promega

G5421

1,000 assays

CellTiter 96® AQueous Non-Radioactive Cell Proliferation Assay

promega

G5430

5,000 assays

CellTiter 96® AQueous Non-Radioactive Cell Proliferation Assay

promega

G5440

50,000 assays

pGEM®-T Easy Vector System I

promega

A1360

20 reactions

pGEM®-T Easy Vector System II

promega

A1380

20 reactions

DeadEnd™ Fluorometric TUNEL System

promega

G3250

60 reactions

DeadEnd™ Colorimetric TUNEL System

promega

G7130

40 reactions

DeadEnd™ Colorimetric TUNEL System

promega

G7360

20 reactions

M-MLV Reverse Transcriptase

promega

M1701

10,000u

M-MLV Reverse Transcriptase

promega

M1705

50,000u

GoTaq® qPCR Master Mix,

promega

A6001

200 Reactions

GoTaq® qPCR Master Mix,

promega

A6002

1000 Reactions

Wizard® DNA Clean-Up System

promega

A7280

100 preps

SV Total RNA Isolation System

promega

Z3100

50 preps

SV Total RNA Isolation System

promega

Z3101

10 preps

SV Total RNA Isolation System

promega

Z3105

250 preps

CellTiter-Glo® Luminescent Cell Viability Assay

promega

G7570

10ml

CellTiter-Glo® Luminescent Cell Viability Assay

promega

G7571

10 × 10ml

CellTiter-Glo® Luminescent Cell Viability Assay

promega

G7572

100ml

CellTiter-Glo® Luminescent Cell Viability Assay

promega

G7573

10 × 100ml

PepTag® Non-Radioactive PKC Assay

promega

V5330

120 reactions

PepTag® Non-Radioactive cAMP-Dependent Protein Kinase Assay

promega

V5340

120 reactions

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